Spiro compounds

ABSTRACT

Compounds of the formula (I):  
                 
 
     (wherein  
     A is an optionally substituted straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally intervened by oxygen or nitrogen atom;  
     Ar 1  is aryl or heteroaryl, any of which is optionally substituted;  
     n is 0 or 1;  
     R 0  is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A;  
     T, U, V and W are independently nitrogen atom or optionally substituted methine, and at least two of T, U, V and W are said methine group;  
     X is —N(SO 2 R 1 )—, —N(COR 2 )— or —CO—;  
     Y is —C(R 3 )(R 4 )—, —O— or —N(R 5 )—;  
     Z is methine or nitrogen atom) exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, etc., sexual and reproductive dysfunctions, and gastro-intestinal motility disorder.

TECHNICAL FIELD

[0001] The present invention is useful in medical fields. In more detail, spiro compounds of the present invention have an effect as neuropeptide Y receptor antagonists and are useful as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases, and the like.

BACKGROUND ART

[0002] Neuropeptide Y (hereinafter referred to as NPY), a peptide consisting of 36 amino acids, was first isolated from porcine brain by Tatemoto et al in 1982 (NATURE, vol. 296 ,p 659(1982)). NPY is widely distributed in central nervous system and peripheral nervous system, and plays various roles as one of the most abundant peptides in the nervous system. That is, npy acts as an orexigenic substance in the central nervous system and markedly promotes fat accumulation via the mediation of secretion of various hormones or the action of the nervous system. It is known that continuous intracerebroventricular administration of NPY induces obesity and insulin resistance due to these actions (INTERNATIONAL JOURNAL OF OBESITY, vol.19, p.517(1995); Endocrinology, vol.133,p.1753(1993)). It is also known that NPY has central actions such as depression, anxiety, schizophrenia, pain, dementia, circadian rhythm control and the like (DRUGS, vol.52, p.371(1996); THE JOURNAL OF NEUROSCIENCE, vol.18, p.3014(1998)). Furthermore, in the periphery, NPY coexists with norepinephrine in sympathetic-nerve terminals and is related to the tonicity of the sympathetic nervous system. It is known that peripheral administration of NPY causes vasoconstriction and enhances the activities of other vasoconstrictive substances such as norepinephrine (BRITISH JOURNAL OF PHARMACOLOGY, vol.95, p.419(1988)). It is also reported that NPY could participate in the development of cardiac hypertrophy as a result of the sympathetic stimulation (PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, vol.97, p.1595(2000)).

[0003] On the other hand, it is reported that NPY is also involved in the secretory function of sexual hormones and growth hormone, sexual behavior and reproductive function, gastro-intestinal motility, bronchoconstriction, inflammation and alcohol preference (LIFE SCIENCE, vol.55, p.551(1994); THE JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY, vol.101, p.S345(1998); NATURE, vol.396, p.366(1998)).

[0004] NPY has a variety of pharmacological effects resulting from NPY binding to some NPY receptors to which peptide YY and pancreatic polypeptide, which are the analogs of NPY, also bind. It is known that these pharmacological effects of NPY are mediated by the action of at least five receptors with or without synergistic interactions (TRENDS IN NEUROSCIENCES, vol.20, p.294(1997)).

[0005] It is reported that the central effects mediated by NPY Y1 receptor include remarkable orexigenic effect (ENDOCRINOLOGY, vol.137, p.3177(1996); ENDOCRINOLOGY, vol.141, p.1011(2000)). Further, NPY Y1 receptor is reported to be involved in anxiety and pain (NATURE,vol.259, p.528(1993); BRAIN RESEARCH, vol.859, p.361(2000). In addition, the pressor effect mediated by the strong vasoconstrictor action in the periphery is also reported (FEBS LETTERS, vol.362, p.192(1995); NATURE MEDICINE, vol.4, p.722(1998)).

[0006] It is known that the effects mediated by NPY Y2 receptor include an inhibitory effect on the release of various neurotransmitters in the sympathetic nerve endings (BRITISH JOURNAL OF PHARMACOLOGY, vol.102, p.41(1991); SYNAPSE, vol.2, p.299(1988)). In periphery, NPY Y2 causes constriction of blood vessel or vas deferens directly or via the control of release of various neurotransmitters (THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, vol.261, p.863(1992); BRITISH JOURNAL OF PHARMACOLOGY, vol.100, p.190(1990)). Inhibition of lipolysis in adipose tissues is also known (ENDOCRINOLOGY, vol.131, p.1970(1992)). Further, inhibition of ion secretion in the gastro-intestinal tract is reported (BRITISH JOURNAL OF PHARMACOLOGY, vol.101, p.247(1990)). On the other hand, the effects on the central nervous system functions such as memory, anxiety and the like are also known (BRAIN RESEARCH, vol.503, p.73(1989); PEPTIDES, vol.19, p.359(1998)).

[0007] It is reported that NPY Y3 receptor exists mainly in brainstem and heart, and is related to the regulation of blood pressure and heart rate (THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, vol.258, p.633(1991); PEPTIDES, vol.11, p.545(1990)). It is also known that NPY Y3 is involved in the control of catecholamine secretion in adrenal gland (THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, vol.244, p.468(1988); LIFE SCIENCE, vol.50, p.PL7(1992)).

[0008] NPY Y4 receptor has high affinity for pancreatic polypeptide in particular. As for the pharmacological effects of NPY Y4, inhibition of pancreatic exocrine secretion and gastro-intestinal motility is reported (GASTROENTEROLOGY, vol.85, p.1411(1983)). Further, it is reported that NPY enhances the secretion of sexual hormones in the central nervous system (ENDOCRINOLOGY, vol.140, p.5171(1999)).

[0009] As for the effects mediated by NPY Y5 receptor, fat accumulation effects including orexigenic effect are prominent (NATURE, vol. 382, p.168(1996); AMERICAN JOURNAL OF PHYSIOLOGY, vol.277, p.R1428(1999)). It is also reported that the NPY Y5 receptor mediates some CNS effects, such as seizure and epilepsy, or pain and morphine withdrawal symptoms, and the control of circadian rhythm (NATURE MEDICINE, vol.3, p.761(1997); PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, vol.96, p.13518(1999); THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, vol.284, p.633(1998); THE JOURNAL OF NEUROSCIENCE, vol.21, p.5367(2001). In addition, diuretic effect and hypoglicemic effect in the periphery are reported (BRITISH JOURNAL OF PHARMACOLOGY, vol. 120, p.1335(1998); ENDOCRINOLOGY, vol.139, p.3018(1998)). NPY is also reported to enhance cardiac hypertrophy as a result of the sympathetic accentuation (PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, vol.97, p.1595 (2000)).

[0010] The effects of NPY are expressed when NPY binds to the NPY receptors in the central or peripheral nervous system. Therefore, the action of NPY can be prevented by blocking its binding to NPY receptors. For this reason, it is expected that substances antagonize NPY binding to NPY receptors may be useful for the prophylaxis or treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, etc., sexual and reproductive dysfunctions, gastro-intestinal motility disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like. (TRENDS IN PHARMACOLOGICAL SCIENCES, vol.15, p.153(1994); LIFE SCIENCE, vol.55, p.551(1994); DRUGS, vol.52, p.371(1996); THE JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY, vol.101, p.S345(1998); NATURE, vol.396, p.366(1998); THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, vol.284, p.633(1998); TRENDS IN PHARMACOLOGICAL SCIENCES, vol.20, p.104(1999); PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, vol.97, p.1595(2000); THE JOURNAL OF NEUROSCIENCE, vol. 21, p.5367(2001); PHARMACOLOGY & THERAPEUTICS, vol.65, p.397(1995).

[0011] It was recently found that, as a result of the study by the present inventors, certain NPY receptor antagonists are useful for the prophylaxis or treatment of hypercholesterolemia, hyperlipidemia and arteriosclerosis (International application publication WO99/27965).

DISCLOSURE OF THE INVENTION

[0012] The object of the present invention is to provide novel medicines which have NPY antagonistic actions.

[0013] The present inventors have discovered that compounds of the formula (I):

[0014] (wherein

[0015] A is a straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of oxo, amino, lower alkylamino, di-lower alkylamino, hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl and —R^(a), and is optionally intervened by oxygen or nitrogen atom;

[0016] Ar¹ is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar²;

[0017] Ar² is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl;

[0018] n is 0 or 1;

[0019] Q is a single bond or carbonyl;

[0020] R^(a) is lower alkyl which is optionally substituted by a substituent selected from the group consisting of amino, lower alkylamino, di-lower alkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine;

[0021] R⁰ is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A;

[0022] R¹, R² and R⁵ are independently hydrogen, lower alkyl, aralkyl or aryl;

[0023] R³ and R⁴ are independently hydrogen, hydroxy, lower alkyl, aralkyl or aryl;

[0024] T, U, V and W are independently methine or nitrogen atom, said methine being optionally substituted by a substituent-selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, and at least two of T, U, V and W are said methine group;

[0025] X is —N(SO₂R¹)—, —N(COR²)— or —CO—;

[0026] Y is —C(R³)(R⁴)—, —O— or —N(R⁵)—;

[0027] Z is methine or nitrogen atom)

[0028] exhibit NPY antagonistic activities and are useful as agents for treatment of various kinds of diseases related to NPY, thereby completed the present invention.

[0029] The compounds of the present invention (I) are useful as agents for the treatment of various diseases related to NPY, that is, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, etc., sexual and reproductive dysfunctions, gastro-intestinal disorders such as gastro-intestinal motility disorder, respiratory disorders, inflammatory diseases or glaucoma, and the like.

[0030] The compounds of the present invention (I) are particularly useful as agents for the treatment of bulimia, obesity, diabetes and the like.

[0031] The present invention relates to the compounds of the formula (I), or the salts or esters thereof, and the production methods and the use thereof.

[0032] The means of terms used in the present specification are defined, and more detailed description of this invention is described below.

[0033] “Halogen” refers to fluorine, chlorine, bromine and iodine.

[0034] “Lower alkyl” refers to a straight- or branched-chain alkyl group having 1 to 6 carbon atoms, and its examples are methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, hexyl, isohexyl and the like.

[0035] “Halo-lower alkyl” refers to said lower alkyl substituted with identically or differently one, two or more, preferably one to three said halogen at the arbitrary, substitutable position(s), and its examples are fluoromethyl, difluoromethyl, trifluoromethyl, 2-fluoroethyl, 1,2-difluoroethyl, chloromethyl, 2-chloroethyl, 1,2-dichloroethyl, bromomethyl, iodomethyl and the like.

[0036] “Hydroxy-lower alkyl” refers to said lower alkyl substituted with one, two or more, preferably one or two hydroxy at the arbitrary, substitutable position(s), and its examples are hydroxymethyl, 2-hydroxyethyl, 1-hydroxy-1-methylethyl, 1,2-dihydroxyethyl, 3-hydroxypropyl and the like.

[0037] “Cyclo-lower alkyl” refers to a cycloalkyl group having 3 to 6 carbon atoms, and its examples are cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and the like.

[0038] “Lower alkenyl” refers to a straight- or branched-chain alkenyl group having 2 to 6 carbon atoms, and its examples are vinyl, 1-propenyl, 2-propenyl, isopropenyl, 3-butenyl, 2-butenyl, 1-butenyl, 1-methyl-2-propenyl, 1-methyl-l-propenyl, 1-ethyl-l-ethenyl, 2-methyl-2-propenyl, 2-methyl-1-propenyl, 3-methyl-2-butenyl, 4-pentenyl and the like.

[0039] “Lower alkoxy” refers to a straight- or branched-chain alkoxy group having 1 to 6 carbon atoms, and its examples are methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butoxy, isobutoxy, tert-butoxy, pentyloxy, isopentyloxy, hexyloxy, isohexyloxy, and the like.

[0040] “Halo-lower alkoxy” refers to said lower alkoxy substituted with identically or differently one, two or more, preferably one to three said halogen at the arbitrary, substitutable position(s), audits examples are fluoromethoxy, difluoromethoxy, trifluoromethoxy, 2-fluoroethoxy, 1,2-difluoroethoxy, chloromethoxy, 2-chloroethoxy, 1,2-dichloroethoxy, bromomethoxy, iodomethoxy and the like.

[0041] “Lower alkylthio” refers to a straight-or branched-chain alkylthio group having 1 to 6 carbon atoms, and its examples are methylthio, ethylthio, propylthio, isopropylthio, butylthio, sec-butylthio, isobutylthio, tert-butylthio, pentylthio, isopentylthio, hexylthio, isohexylthio and the like.

[0042] “Lower alkanoyl” refers to an alkanoyl group containing said lower alkyl, that is, an alkanoyl group having 2 to 7 carbon atoms, and its examples are acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, pivaloyl and the like.

[0043] “Lower alkoxycarbonyl” refers to an alkoxycarbonyl group containing said lower alkoxy, that is, an alkoxycarbonyl group having 2 to 7 carbon atoms, and its examples are methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl, butoxycarbonyl, isobutoxycarbonyl, tert-butoxycarbonyl, pentyloxycarbonyl and the like.

[0044] “Aryl” refers to phenyl, naphthyl and the like.

[0045] “Heteroaryl” refers to 5- or 6-membered monocyclic heteroaromatic group which contains one, two or more, preferably one to three hetero atom(s) identically or differently selected from the group consisting of oxygen, nitrogen and sulfur; or condensed cyclic heteroaromatic group, where said monocyclic heteroaromatic group is condensed with said aryl group or condensed each other with the same or different said monocyclic heteroaromatic group, and its examples are pyrrolyl, furyl, thienyl, imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, tetrazolyl, oxadiazolyl, 1,2,3-thiadiazolyl, 1,2,4-thiadiazolyl, 1,3,4-thiadiazolyl, pyridyl, pyrazinyl, pyrimidinyl, pyridazinyl, 1,2,4-triazinyl, 1,3,5-triazinyl, indolyl, benzofuranyl, benzothienyl, benzoimidazolyl, benzoxazolyl, benzoisoxazolyl, benzothiazolyl, benzoisothiazolyl, indazolyl, purinyl, quinolyl, isoquinolyl, phthalazinyl, naphthylidinyl, quinoxalinyl, quinazolinyl, cinnolinyl, pteridinyl, pyrido[3,2-b]pyridyl and the like.

[0046] “A straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally intervened by oxygen or nitrogen atom” refers to a saturated or unsaturated straight-chain hydrocarbon having 1 to 6 carbon atoms, which may or may not be intervened by one, two or more, preferably one oxygen or nitrogen atom(s), at the arbitrary position(s) capable of being intervened, and examples thereof are methylene, ethylene, trimethylene, tetramethylene, pentamethylene, 1-azatrimethylene, 1-azatetramethylene, 2-azatetramethylene, 2-oxatetramethylene, 2-oxapentamethylene, 3-oxapentamethylene and the like.

[0047] “Lower alkylamino” refers to an amino group mono-substituted with said lower alkyl, and its examples are methylamino, ethylamino, propylamino, isopropylamino, butylamino, sec-butylamino, tert-butylamino and the like.

[0048] “Di-lower alkylamino” refers to an amino group di-substituted with identical or different said lower alkyl, and its examples are dimethylamino, diethylamino, ethylmethylamino, dipropylamino, methylpropylamino, diisopropylamino and the like.

[0049] “Lower alkylene” refers to a straight- or branched-chain alkylene group having 1 to 6 carbon atoms, and its examples are methylene, ethylene, trimethylene, tetramethylene, pentamethylene, hexamethylene and the like.

[0050] “Aralkyl” refers to said lower alkyl substituted with one, two or more, preferably one or two aryl at the arbitrary, substitutable position(s), and its examples are benzyl, 2-phenylethyl, 3-phenylethyl, 1-phenylethyl and the like.

[0051] The salts of the compounds of the formula (I) refer to the pharmaceutically acceptable, common salts, and examples thereof are base addition salt to said carboxyl group when the compound has a carboxyl group, or acid addition salt to an amino or said basic heterocyclyl when the compound has a basic heterocyclyl group, and the like.

[0052] Said base addition salts include salts with alkali metals (e.g. sodium, potassium); salts with alkaline earth metals (e.g. calcium, magnesium); ammonium salts; salts with organic amines (e.g. trimethylamine, triethylamine, dicyclohexylamine, ethanolamine, diethanolamine, triethanolamine, procaine, N,N′-dibenzylethylenediamine) and the like.

[0053] Said acid addition salts include salts with inorganic acids (e.g. hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid, perchloric acid), salts with organic acids (e.g. maleic acid, fumaric acid, tartaric acid, citric acid, ascorbic acid, trifluoroacetic acid), salts with sulfonic acids (e.g. methanesulfonic acid, isethionic acid, benzenesulfonic acid, p-toluenesulfonic acid) and the like.

[0054] The esters of the compounds of the formula (I) refer to, for example, the pharmaceutically acceptable, common esters of said carboxyl group when the compound has a carboxyl group, and examples thereof are esters with lower alkyl (e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, cyclopropyl, cyclobutyl, cyclopentyl), esters with aralkyl (e.g. benzyl, phenethyl), esters with lower alkenyl (e.g. allyl, 2-butenyl), esters with lower-alkoxy-lower-alkyl (e.g. methoxymethyl, 2-methoxyethyl, 2-ethoxyethyl), esters with lower-alkanoyloxy-lower-alkyl (e.g. acetoxymethyl, pivaloyloxymethyl, 1-pivaloyloxyethyl), esters with lower-alkoxycarbonyl-lower-alkyl (e.g. methoxycarbonylmethyl, isopropoxycarbonylmethyl), esters with carboxy-lower alkyl (e.g. carboxymethyl), esters with lower-alkoxycarbonyloxy-lower-alkyl (e.g. 1-(ethoxycarbonyloxy)ethyl, 1-(cyclohexyloxycarbonyloxy)ethyl), esters with carbamoyloxy-lower alkyl (e.g. carbamoyloxymethyl), esters with phthalidyl, esters with (5-substituted-2-oxo-1,3-dioxol-4-yl)methyl (e.g. (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl) and the like.

[0055] “An agent for treatment” refers to a medicament which is employed for the treatment and/or prophylaxis of various diseases.

[0056] In order to disclose the aforesaid compounds of the formula (I) of the present invention more specifically, the various symbols used in the formula (I) are explained in more detail by presenting preferred embodiments.

[0057] A refers to a straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of oxo, amino, lower alkylamino, di-lower alkylamino, hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl and —R^(a), and is optionally intervened by oxygen or nitrogen atom.

[0058] “A straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of oxo, amino, lower alkylamino, di-lower alkylamino, hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl and —R^(a), and is optionally intervened by oxygen or nitrogen atom” refers to unsubstituted said straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally intervened by oxygen or nitrogen atom; or said straight-chain hydrocarbon having 1 to 6 carbon atoms, which has substituent(s) at the arbitrary, substitutable position(s), and is optionally intervened by oxygen or nitrogen atom, wherein said substituent may be one, two or more member(s), preferably one member identically or differently selected from the group consisting of oxo, amino, lower alkylamino, di-lower alkylamino, hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl and —R^(a).

[0059] The preferable examples of lower alkylamino as said substituent include methylamino, ethylamino, propylamino and the like.

[0060] The preferable examples of di-lower alkylamino as said substituent include dimethylamino, diethylamino and the like.

[0061] The preferable examples of lower alkoxy as said substituent include methoxy, ethoxy, propoxy and the like.

[0062] The preferable examples of lower alkoxycarbonyl as said substituent include methoxycarbonyl, ethoxycarbonyl and the like.

[0063] The preferable examples of lower alkylene as said substituent include methylene, ethylene, trimethylene and the like.

[0064] The preferable examples of aryl as said substituent include phenyl, naphthyl and the like.

[0065] The preferable examples of heteroaryl as said substituent include pyridyl, quinolyl, indolyl and the like.

[0066] A group represented by the formula: —R^(a) as said substituent refers to lower alkyl which is optionally substituted by a substituent selected from the group consisting of amino, lower alkylamino, di-lower alkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine.

[0067] “Lower alkyl which is optionally substituted by a substituent selected from the group consisting of amino, lower alkylamino, di-lower alkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine” refers to unsubstituted said lower alkyl, or said lower alkyl having substituent(s) at the arbitrary, substitutable position(s), wherein said substituent may be one, two or more, preferably one member(s) identically or differently selected from the group consisting of amino, lower alkylamino, di-lower alkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine.

[0068] The preferable examples of lower alkylamino as said substituent include methylamino, ethylamino, propylamino and the like.

[0069] The preferable examples of di-lower alkylamino as said substituent include dimethylamino, diethylamino and the like.

[0070] The preferable examples of cyclo-lower alkyl being optionally substituted by fluorine as said substituent include cyclopentyl, cyclohexyl and the like.

[0071] The preferable examples of aryl being optionally substituted by fluorine as said substituent include phenyl, 4-fluorophenyl, naphthyl and the like.

[0072] The preferable examples of heteroaryl being optionally substituted by fluorine as said substituent include pyridyl, quinolyl, indolyl and the like.

[0073] The preferable examples of lower alkyl of “lower alkyl which is optionally substituted” as R^(a) include methyl, ethyl, propyl and the like.

[0074] The preferable examples of R^(a) include hydroxymethyl, cyclohexylmethyl, benzyl, 4-fluorobenzyl, 3-pyridylmethyl, 4-pyridylmethyl, 3-indolylmethyl and the like.

[0075] The preferable examples of substituent of A include oxo, hydroxy, lower alkoxycarbonyl, lower alkylene, aryl, —R^(a) and the like.

[0076] To be more specific, A includes, for example, a group of the formula (A-1) and (A-2):

[0077] and the like.

[0078] Ar¹ is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar².

[0079] “Aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar²” refers to unsubstituted said aryl or said heteroaryl, or said aryl or said heteroaryl, the last two groups having substituent(s) at the arbitrary, substitutable position(s) wherein said substituent may be one, two or more, preferably one or two member(s) identically or differently selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar².

[0080] The preferable examples of halogen as said substituent include fluorine, chlorine and the like.

[0081] The preferable examples of lower alkyl as said substituent include methyl, ethyl, propyl, isopropyl and the like.

[0082] The preferable examples of halo-lower alkyl as said substituent include difluoromethyl, trifluoromethyl and the like.

[0083] The preferable examples of hydroxy-lower alkyl as said substituent include hydroxymethyl, 2-hydroxyethyl, 1-hydroxy-methylethyl and the like.

[0084] The preferable examples of cyclo-lower alkyl as said substituent include cyclopropyl, cyclobutyl and the like.

[0085] The preferable examples of lower alkenyl as said substituent include vinyl, 1-propenyl, 2-methyl-1-propenyl and the like.

[0086] The preferable examples of lower alkoxy as said substituent include methoxy, ethoxy and the like

[0087] The preferable examples of halo-lower alkoxy as said substituent include fluoromethoxy, difluoromethoxy, trifluoromethoxy and the like.

[0088] The preferable examples of lower alkylamino as said substituent include methylamino, ethylamino, propylamino and the like.

[0089] The preferable examples of di-lower alkylamino as said substituent include dimethylamino, diethylamino and the like.

[0090] The preferable examples of lower alkylthio as said substituent include methylthio, ethylthio and the like.

[0091] The preferable examples of lower alkanoyl as said substituent include acethyl, propionyl and the like.

[0092] The preferable examples of lower alkoxycarbonyl as said substituent include methoxycarbonyl, ethoxycarbonyl and the like.

[0093] In a group represented by the formula: -Q-Ar² as said substituent, Ar² is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl; Q is a single bond or carbonyl.

[0094] “Aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl” refers to unsubstituted said aryl or said heteroaryl, or said aryl or said heteroaryl, the last two groups having substituent(s) at the arbitrary, substitutable position(s) wherein said substituent may be one, two or more, preferably one or two member(s) identically or differently selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy- lower alkyl, hydroxy, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl.

[0095] The preferable examples of halogen as said substituent include fluorine, chlorine and the like.

[0096] The preferable examples of lower alkyl as said substituent include methyl, ethyl, propyl, isopropyl and the like.

[0097] The preferable examples of halo-lower alkyl as said substituent include difluoromethyl, trifluoromethyl and the like.

[0098] The preferable examples of hydroxy-lower alkyl as said substituent include hydroxymethyl, 2-hydroxyethyl, 1-hydroxy-1-methylethyl and the like.

[0099] The preferable examples of lower alkoxy as said substituent include methoxy, ethoxy and the like.

[0100] The preferable examples of halo-lower alkoxy as said substituent include fluoromethoxy, difluoromethoxy, trifluoromethoxy and the like.

[0101] The preferable examples of lower alkylamino as said substituent include methylamino, ethylamino and the like.

[0102] The preferable examples of di-lower alkylamino as said substituent include dimethylamino, diethylamino and the like.

[0103] The preferable examples of lower alkanoyl as said substituent include acetyl, propionyl and the like.

[0104] The preferable examples of aryl as said substituent include phenyl and the like.

[0105] The preferable examples of the substituent of Ar² include halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, halo-lower alkoxy and the like.

[0106] The preferable examples of aryl as Ar² include phenyl and the like, and preferred examples of heteroaryl as Ar² include imidazolyl, pyridyl, benzofuranyl, quinolyl and the like.

[0107] Thus, the preferable examples of a group represented by the formula: -Q-Ar² include phenyl, 2-fluorophenyl,, 3-fluorophenyl, 4-fluorophenyl, 2,3-difluorophenyl, 2,4-difluorophenyl, 3,5-difluorophenyl, 2-chlorophenyl, 3-chlorophenyl, 4-chlorophenyl, 2-cyanophenyl, 3-cyanophenyl, 4-cyanophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-fluoro-5-methylphenyl, 3-fluoromethylphenyl, 2-trifluoromethylphenyl, 3-trifluoromethylphenyl, 4-trifluoromethylphenyl, 2-methoxyphenyl, 3-methoxyphenyl, 4-methoxyphenyl, 3-fluoro-5-methoxyphenyl, 3-fluoromethoxyphenyl, 3-difluoromethoxyphenyl, 3-(2-hydroxyethyl)phenyl, 3-hydroxymethylphenyl, 3-(1-hydroxy-1-methylethyl)phenyl, 3-hydroxyphenyl, 4-hydroxyphenyl, 2-imidazolyl, 1-ethyl-2-imidazolyl, 1,2,4-thiadiazol-5-yl, 1,3,4-thiadiazol-2-yl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-ethyl-4-pyridyl, 4-pyrimidinyl, 5-pyrimidinyl, 4-benzo[b]furanyl, 5-benzo[b]furanyl, 7-benzo[b]furanyl, 2-quinolyl, 3-quinolyl, 4-quinolyl, 5-quinolyl, 6-quinolyl, 8-quinolyl, benzoyl, 2-pyridylcarbonyl and the like, among which the more preferable examples are phenyl, 2-fluorophenyl, 3-fluorophenyl, 3,5-difluorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3-cyanophenyl, 3-trifluoromethylphenyl, 3-difluoromethoxyphenyl, 3-(2-hydroxyethyl)phenyl, 3-hydroxyphenyl, 4-hydroxyphenyl, 1-ethyl-2-imidazolyl, 2-pyridyl, 7-benzo[b]furanyl, 2-quinolyl, 3-quinolyl, benzoyl, 2-pyridylcarbonyl and the like.

[0108] The preferable examples of the substituent of Ar¹ include halogen, lower alkyl, halo-lower alkyl, lower alkenyl, lower alkoxy, di-lower alkylamino, lower alkanoyl, -Q-Ar²and the like, more preferably, halogen, halo-lower alkyl, lower alkoxy, di-lower alkylamino and the like.

[0109] The preferable examples of aryl as Ar¹ preferably include phenyl and the like, and the preferable examples of heteroaryl as Ar¹ preferably include imidazolyl, pyrazolyl, thiazolyl, oxazolyl, isoxazolyl, 1,2,4-thiadiazolyl, pyridyl, pyrazinyl, pyrimidinyl, 1,2,4-triazinyl, benzoxazolyl, benzothiazolyl, quinolyl, pyrido[3,2-b]pyridyl and the like, more preferably, pyridyl and the like.

[0110] R⁰ refers to hydrogen, or lower alkylene attached to an arbitrary, bondable position of A.

[0111] The preferable examples of lower alkylene as R⁰ include methylene, ethylene, trimethylene, tetramethylene and the like.

[0112] Thus, a group represented by the formula: -A-Ar¹—R⁰ includes, for example, 1-phenyl-3-pyrrolidinyl, 1-(2-fluorophenyl)-3-pyrrolidinyl, 1-(3-fluorophenyl)-3-pyrrolidinyl, 1-(4-fluorophenyl)-3-pyrrolidinyl, 1-(2-pyridyl)-3-pyrrolidinyl, 1-(3-pyridyl)-3-pyrrolidinyl, 1-(4-pyridyl)-3-pyrrolidinyl, 1-(3,5-difluorophenyl)-3-pyrrolidinyl, 1-(3-trifluoromethylphenyl)-3-pyrrolidinyl, 1-(2-pyrimidinyl)-3-pyrrolidinyl, 5-oxo-1-phenyl-3-pyrrolidinyl, 1-phenyl-4-piperidyl, 1-(2-fluorophenyl)-4-piperidyl, 1-(3-fluorophenyl)-4-piperidyl, 1-(4-fluorophenyl)-4-piperidyl, 1-(3,5-difluorophenyl)-4-piperidyl, 1-(2-pyridyl)-4-piperidyl, 1-(3-pyridyl)-4-piperidyl, 1-(4-pyridyl)-4-piperidyl, 3-hydroxymethyl-1-phenyl-4-piperidyl, 3-methoxycarbonyl-1-phenyl-4-piperidyl, 3-ethoxycarbonyl-1-phenyl-4-piperidyl, 3-isopropoxycarbonyl-1-phenyl-4-piperidyl, 1-phenyl-3-piperidyl, 1-(2-fluorophenyl)-3-piperidyl, 1-(3-fluorophenyl)-3-piperidyl, 1-(4-fluorophenyl)-3-piperidyl, 1-(3,5-difluorophenyl)-3-piperidyl, 1-(2-pyridyl)-3-piperidyl, 1-(3-pyridyl)-3-piperidyl, 1-(4-pyridyl)-3-piperidyl, 3-phenylcyclopentyl, 3-phenylcyclohexyl, 4-phenylcyclohexyl, 4-(2-fluorophenyl)cyclohexyl, 4-(3-fluorophenyl)cyclohexyl, 4-(4-fluorophenyl)cyclohexyl, 4-(2-pyridyl)cyclohexyl, 4-(3-pyridyl)cyclohexyl, 4-(4-pyridyl)cyclohexyl, 4-(4-fluoro-3-pyridyl)cyclohexyl, 4-(3-quinolyl)cyclohexyl, 4-(3-fluorophenyl)-4-hydroxycyclohexyl, 6-phenyl-3-tetrahydropyranyl, 6-(3-fluorophenyl)-3-tetrahydropyranyl, 2-phenylcyclopropyl, 2-(2-pyridyl)cyclopropyl, 2-(3-pyridyl)cyclopropyl, 2-(4-pyridyl)cyclopropyl, 2-indanyl, 2-tetrahydronaphthyl, 6-methoxy-2-tetrahydronaphthyl, benzyl, phenethyl, 3-phenylpropyl, 4-phenylbutyl, 4-bromophenethyl, 3-methoxyphenethyl, 2-propyloxyphenethyl, 4-dimethylaminophenethyl, 3,5-difluorophenethyl, 3,4-dimethoxyphenethyl, 4-(dimethylamino)-2-methoxyphenethyl, 2-(3-quinolyl)ethyl, 2-hydroxy-2-(3-quinolyl)ethyl, 2-hydroxy-2-phenylethyl, benzoylmethyl, 2-hydroxy-2-(4-dimethylaminophenyl)ethyl, 2-hydroxy-2-(3,5-difluorophenyl)ethyl, 1-(hydroxymethyl)-2-phenylethyl, 1-(methoxycarbonyl)-2-phenylethyl, 1-(aminomethyl)-2-phenylethyl, 1-(isobutylaminomethyl)-2-phenylethyl, 1-benzyl-2-(benzylamino)ethyl, 1-benzyl-2-anilinoethyl, 1-benzyl-2-(2-pyridylmethylamino)ethyl, 1-benzyl-2-(3-pyridylmethylamino)ethyl, 1-benzyl-2-(N-benzyl-N-methylamino)ethyl, 1-benzyl-2-(benzyloxy)ethyl, 1-(cyclohexylmethyl)-2-(benzyloxy)ethyl, 1-benzyloxycarbonyl-2-cyclohexylethyl, 1-(benzyloxycarbonyl)-2-(3-indolyl)ethyl, 1-(benzylcarbamoyl)-2-phenylethyl, 1-(benzylcarbamoyl)-2-cyclohexylethyl, 1-(benzylcarbamoyl)-2-(4-pyridyl)ethyl, 1-(4-pyridylmethylcarbamoyl)-2-(4-fluorophenyl)ethyl, 1-(N-methylbenzylcarbamoyl)-2-phenylethyl, 1-(N-methylbenzylcarbamoyl)-2-(3-pyridyl)ethyl and the like, among which the more preferable examples are 1-phenyl-3-pyrrolidinyl, 1-(2-fluorophenyl)-3-pyrrolidinyl, 1-(3-fluorophenyl)-3-pyrrolidinyl, 1-(4-fluorophenyl)-3-pyrrolidinyl, 1-phenyl-4-piperidyl, 1-(2-fluorophenyl)-4-piperidyl, 1-(3-fluorophenyl)-4-piperidyl, 1-(3,5-difluorophenyl)-4-piperidyl, 4-phenylcyclohexyl, 4-(2-fluorophenyl)cyclohexyl, 4-(3-fluorophenyl)cyclohexyl, 4-dimethylaminophenethyl, 1-benzyl-2-(benzylamino)ethyl, 1-benzyl-2-(2-pyridylmethylamino)ethyl, 1-benzyl-2-(3-pyridylmethylamino)ethyl, 1-benzyl-2-(benzyloxy)ethyl, 1-(benzylcarbamoyl)-2-phenylethyl, 1-(benzylcarbamoyl)-2-(4-pyridyl)ethyl and the like.

[0113] n is 0 or 1, preferably 0.

[0114] T, U, V and W are independently methine or nitrogen atom, said methane being optionally substituted by a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, and at least two of T, U, V and W are said methine group;

[0115] “Methine being optionally substituted by a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy” refers to unsubstituted methine or methine having a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy.

[0116] The preferable examples of halogen as said substituent include fluorine, chlorine and the like.

[0117] The preferable examples of lower alkyl as said substituent include methyl, ethyl and the like.

[0118] The preferable examples of lower alkoxy as said substituent include methoxy, ethoxy and the like.

[0119] The preferable examples of the said substituent include halogen atom and the like.

[0120] The preferred embodiments of T, U, V and W include the case where T, U, V and W are independently methine optionally having said substituent, preferably halogen; or the case where one of T, U, V and W is nitrogen atom; and the like.

[0121] X is —N(SO₂R¹)—, —N(COR²)— or —CO—;

[0122] Y is —C(R³)(R⁴)—, —O— or —N(R⁵)—;

[0123] R¹, R² and R⁵ are independently hydrogen, lower alkyl, aralkyl or aryl;

[0124] R³ and R⁴ are independently hydrogen, hydroxy, lower alkyl, aralkyl or aryl.

[0125] The preferable examples of lower alkyl as R¹, R², R³, R⁴ or R⁵ include each independently methyl, ethyl, propyl and the like.

[0126] The preferable examples of aralkyl as R¹, R², R³, R⁴ or R⁵ include each independently benzyl and the like.

[0127] The preferable examples of aryl as R¹, R², R³, R⁴ or R⁵ include each independently phenyl and the like.

[0128] The preferable examples of R¹ and R² include lower alkyl and the like.

[0129] The preferred embodiments of R³ and R⁴ are the case where both R³ and R⁴ are hydrogen, and the like.

[0130] The preferable examples of R⁵ include hydrogen, lower alkyl and the like, more preferably hydrogen and the like.

[0131] The preferred embodiment of X, Y and n includes, for example, the case where X is —N(SO₂R¹)— or —N(COR²)—, preferably —N(SO₂R¹)—, n is 0, and Y is —C(R³)(R⁴)—; or the case where X is —CO—, and Y is —O— or —N(R⁵)—, more preferably —O—, and among which the case where X is —CO— and Y is —O— or —NH—; and the case where X is —CO— and Y is —O— are more preferable.

[0132] Z is methine or nitrogen atom, preferably methine.

[0133] In more detail, the preferable examples of a group of the formula (VII):

[0134] include a group represented by the following formulas (VIII):

[0135] (wherein R¹ has the same meaning as defined above) and the like.

[0136] Preferred compounds of the formula (I) are, for example, compounds of the formula (I-a):

[0137] wherein A, Ar¹, R⁰ and R¹ have the same meaning as defined above, compounds of the formula (I-b):

[0138] wherein A, Ar¹, R⁰ and R¹ have the same meaning as defined above, compounds of the formula (I-c):

[0139] wherein A, Ar¹ and R⁰ have the same meaning as defined above, compounds of the formula (I-d):

[0140] wherein A, Ar¹, R⁰, T, U, V and W have the same meaning as defined above, and compounds of the formula (I-e):

[0141] wherein A, Ar¹ and R⁰ have the same meaning as defined above.

[0142] Preferred compounds of the formula (I-d) are, for example, compounds wherein all of T, U, V and W are unsubstituted methine, or compounds wherein one of T, U, V and W is nitrogen atom.

[0143] Preferred compounds of the formula (I), (I-a), (I-b), (I-c), (I-d) or (I-e) are, for example, compounds wherein aryl as Ar¹ is phenyl, or compounds wherein Ar¹ is heteroaryl which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar².

[0144] The compounds of the present invention may include stereoisomers such as optical isomers, diastereoisomers and geometrical isomers, or tautomers depending upon the mode of substituents. The compounds of the present invention include all the stereoisomers, tautomers and their mixtures.

[0145] For example, compounds of the formula (I-b) include stereoisomers such as trans-form compound of the formula (I-1b):

[0146] and cis-form compound of the formula (I-2b):

[0147] among which trans-form compound is preferred.

[0148] Also, compounds of the formula (I-d) include stereoisomers such as trans-form compound of the formula (I-1d):

[0149] and cis-form compound of the formula (I-2d):

[0150] among which trans-form compound is preferred.

[0151] Also included within the scope of the invention are polymorphs, hydrates and solvates of the compounds of the present invention.

[0152] The present invention also includes prodrugs of the compounds of the present invention within its scope. In general, such prodrugs are functional derivatives of the compounds of the present invention which can be readily converted in vivo into the required compound. Thus, in the treatment methods for various diseases according to the present invention, the term “administering” shall encompass not only administration of the compound specified in this disclosure but also administration of a compound which is converted in vivo into the specified compound when it is administered to a patient. Conventional procedures for selection and preparation of suitable prodrug derivatives are described, for example, in “Design of Prodrugs,” ed. H. Bundgaard, Elsevier (1985), which are referred and entirely incorporated in this specification. The metabolites of these compounds include active compounds which are produced upon introduction of compounds of the present invention into the biological milieu, and they are encompassed in the scope of the present invention.

[0153] The specific compounds of the formula (I) are, for example, following compounds.

[0154] In the tables, Me refers to methyl group, and Et refers to ethyl group. TABLE 1

No. R¹ Z A—Ar¹—R⁰ 1 Me CH 1-phenyl-3-pyrrolidinyl 2 Me CH 1-(2-fluorophenyl)-3-pyrrolidinyl 3 Me CH 1-(3-fluorophenyl)-3-pyrrolidinyl 4 Me CH 1-(4-fluorophenyl)-3-pyrrolidinyl 5 Me CH 1-(2-chlorophenyl)-3-pyrrolidinyl 6 Me CH 1-(3-chlorophenyl)-3-pyrrolidinyl 7 Me CH 1-(4-chlorophenyl)-3-pyrrolidinyl 8 Me CH 1-(2-methylphenyl)-3-pyrrolidinyl 9 Me CH 1-(3-methylphenyl)-3-pyrrolidinyl 10 Me CH 1-(4-methylphenyl)-3-pyrrolidinyl 11 Me CH 1-(2-methoxyphenyl)-3-pyrrolidinyl 12 Me CH 1-(3-methoxyphenyl)-3-pyrrolidinyl 13 Me CH 1-(4-methoxyphenyl)-3-pyrrolidinyl 14 Me CH 1-(2-trifluoromethylphenyl)-3-pyrrolidinyl 15 Me CH 1-(3-trifluoromethylphenyl)-3-pyrrolidinyl 16 Me CH 1-(4-trifluoromethylphenyl)-3-pyrrolidinyl 17 Me CH 1-(3,5-difluorophenyl)-3-pyrrolidinyl 18 Me CH 1-(2-difluoromethoxyphenyl)-3-pyrrolidinyl 19 Me CH 1-(3-difluoromethoxyphenyl)-3-pyrrolidinyl 20 Me CH 1-(4-difluoromethoxyphenyl)-3-pyrrolidinyl 21 Me CH 1-(2-pyridyl)-3-pyrrolidinyl 22 Me CH 1-(3-pyridyl)-3-pyrrolidinyl 23 Me CH 1-(4-pyridyl)-3-pyrrolidinyl 24 Me CH 1-(2-pyrimidinyl)-3-pyrrolidinyl 25 Me CH 5-oxo-1-phenyl-3-pyrrolidinyl 26 Me CH 1-phenyl-3-piperidyl 27 Me CH 1-(2-fluorophenyl)-3-piperidyl 28 Me CH 1-(3-fluorophenyl)-3-piperidyl 29 Me CH 1-(4-fluorophenyl)-3-piperidyl 30 Me CH 1-(2-chlorophenyl)-3-piperidyl 31 Me CH 1-(3-chlorophenyl)-3-piperidyl 32 Me CH 1-(4-chlorophenyl)-3-piperidyl 33 Me CH 1-(2-methylphenyl)-3-piperidyl 34 Me CH 1-(3-methylphenyl)-3-piperidyl 35 Me CH 1-(4-methylphenyl)-3-piperidyl 36 Me CH 1-(2-methoxyphenyl)-3-piperidyl 37 Me CH 1-(3-methoxyphenyl)-3-piperidyl 38 Me CH 1-(4-methoxyphenyl)-3-piperidyl 39 Me CH 1-(2-trifluoromethylphenyl)-3-piperidyl 40 Me CH 1-(3-trifluoromethylphenyl)-3-piperidyl 41 Me CH 1-(4-trifluoromethylphenyl)-3-piperidyl 42 Me CH 1-(3,5-difluorophenyl)-3-piperidyl 43 Me CH 1-(2-difluoromethoxyphenyl)-3-piperidyl 44 Me CH 1-(3-difluoromethoxyphenyl)-3-piperidyl 45 Me CH 1-(4-difluoromethoxyphenyl)-3-piperidyl 46 Me CH 1-(2-pyridyl)-3-piperidyl 47 Me CH 1-(3-pyridyl)-3-piperidyl 48 Me CH 1-(4-pyridyl)-3-piperidyl 49 Me CH 1-phenyl-4-piperidyl 50 Me CH 1-(2-fluorophenyl)-4-piperidyl 51 Me CH 1-(3-fluorophenyl)-4-piperidyl 52 Me CH 1-(4-fluorophenyl)-4-piperidyl 53 Me CH 1-(2-chlorophenyl)-4-piperidyl 54 Me CH 1-(3-chlorophenyl)-4-piperidyl 55 Me CH 1-(4-chlorophenyl)-4-piperidyl 56 Me CH 1-(2-methylphenyl)-4-piperidyl 57 Me CH 1-(3-methylphenyl)-4-piperidyl 58 Me CH 1-(4-methylphenyl)-4-piperidyl 59 Me CH 1-(2-methoxyphenyl)-4-piperidyl 60 Me CH 1-(3-methoxyphenyl)-4-piperidyl 61 Me CH 1-(4-methoxyphenyl)-4-piperidyl 62 Me CH 1-(2-trifluoromethylphenyl)-4-piperidyl 63 Me CH 1-(3-trifluoromethylphenyl)-4-piperidyl 64 Me CH 1-(4-trifluoromethylphenyl)-4-piperidyl 65 Me CH 1-(3,5-difluorophenyl)-4-piperidyl 66 Me CH 1-(2-difluoromethoxyphenyl)-4-piperidyl 67 Me CH 1-(3-difluoromethoxyphenyl)-4-piperidyl 68 Me CH 1-(4-difluoromethoxyphenyl)-4-piperidyl 69 Me CH 1-(2-pyridyl)-4-piperidyl 70 Me CH 1-(3-pyridyl4-4-piperidyl 71 Me CH 1-(4-pyridyl)-4-piperidyl 72 Me CH 3-hydroxymethyl-1-phenyl-4-piperidyl 73 Me CH 3-methoxycarbonyl-1-phenyl-4-piperidyl 74 Me CH 3-ethoxycarbonyl-1-phenyl-4-piperidyl 75 Me CH 3-isopropoxycarbonyl-1-phenyl-4-piperidyl 76 Me CH 4-phenylcyclohexyl 77 Me CH 4-(2-fluorophenyl)cyclohexyl 78 Me CH 4-(3-fluorophenyl)cyclohexyl 79 Me CH 4-(4-fluorophenyl)cyclohexyl 80 Me CH 4-(2-chlorophenyl)cyclohexyl 81 Me CH 4-(3-chlorophenyl)cyclohexyl 82 Me CH 4-(4-chlorophenyl)cyclohexyl 83 Me CH 4-(2-methylphenyl)cyclohexyl 84 Me CH 4-(3-methylphenyl)cyclohexyl 85 Me CH 4-(4-methylphenyl)cyclohexyl 86 Me CH 4-(2-methoxyphenyl)cyclohexyl 87 Me CH 4-(3-methoxyphenyl)cyclohexyl 88 Me CH 4-(4-methoxyphenyl)cyclohexyl 89 Me CH 4-(2-trifluoromethylphenyl)cyclohexyl 90 Me CH 4-(3-trifluoromethylphenyl)cyclohexyl 91 Me CH 4-(4-trifluoromethylphenyl)cyclohexyl 92 Me CH 4-(3,5-difluorophenyl)cyclohexyl 93 Me CH 4-(3-acetylphenyl)cyclohexyl 94 Me CH 4-(3-cyanophenyl)cyclohexyl 95 Me CH 4-(2-difluoromethoxyphenyl)cyclohexyl 96 Me CH 4-(3-difluoromethoxyphenyl)cyclohexyl 97 Me CH 4-(4-difluoromethoxyphenyl)cyclohexyl 98 Me CH 4-(2-pyridyl)cyclohexyl 99 Me CH 4-(3-pyridyl)cyclohexyl 100 Me CH 4-(4-pyridyl)cyclohexyl 101 Me CH 4-(4-fluoro-3-pyridyl)cyclohexyl 102 Me CH 4-(3-quinolyl)cyclohexyl 103 Me CH 4-(3-fluorophenyl)-4-hydroxycyclohexyl 104 Me CH 3-phenylcyclohexyl 105 Me CH 3-phenylcyclopentyl 106 Me CH 6-phenyl-3-tetrahydropyranyl 107 Me CH 6-(3-fluorophenyl)-3-tetrahydropyranyl 108 Me CH 2-phenylcyclopropyl 109 Me CH 2-(2-pyridyl)cyclopropyl 110 Me CH 2-(3-pyridyl)cyclopropyl 111 Me CH 2-(4-pyridyl)cyclopropyl 112 Me CH 2-(3-fluorophenyl)cyclopropyl 113 Me CH 2-indanyl 114 Me CH 2-tetrahydronaphthyl 115 Me CH 6-methoxy-2-tetrahydronaphthyl 116 Me CH benzyl 117 Me CH phenethyl 118 Me CH 3-phenylpropyl 119 Me CH 4-phenylbutyl 120 Me CH 2-methoxyphenethyl 121 Me CH 3-methoxyphenethyl 122 Me CH 4-methoxyphenethyl 123 Me CH 4-fluorophenethyl 124 Me CH 4-bromophenethyl 125 Me CH 4-chlorophenethyl 126 Me CH 3-trifluoromethylphenethyl 127 Me CH 3,4-dimethoxyphenethyl 128 Me CH 3-propoxyphenethyl 129 Me CH 3,5-difluorophenethyl 130 Me CH 4-dimethylaminophenethyl 131 Me CH 3-difluoromethoxyphenethyl 132 Me CH 2-methylphenethyl 133 Me CH 4-acetylphenethyl 134 Me CH 4-dimethylamino-2-methoxyphenethyl 135 Me CH cyclohexylethyl 136 Me CH 2-(2-pyridyl)ethyl 137 Me CH 2-(3-pyridyl)ethyl 138 Me CH 2-(4-pyridyl)ethyl 139 Me CH 2-(2-quinolyl)ethyl 140 Me CH 2-(3-quinolyl)ethyl l41 Me CH 2-(4-quinolyl)ethyl 142 Me CH 2-(6-quinolyl)ethyl 143 Me CH 2-(2-indolyl)ethyl 144 Me CH 2-(3-indolyl)ethyl 145 Me CH 2-(7-aza-3-indolyl)ethyl 146 Me CH 2-(benzimidazolyl)ethyl 147 Me CH 2-(benzoxazolyl)ethyl 148 Me CH 2-(benzothiazolyl)ethyl 149 Me CH 2-(1-naphthyl)ethyl 150 Me CH 2-(2-naphthyl)ethyl 151 Me CH 1-(hydroxymethyl)-2-phenylethyl 152 Me CH 1-(methoxycarbonyl)-2-phenylethyl 153 Me CH 1-(ethoxycarbonyl)-2-phenylethyl 154 Me CH 1-carboxy-2-phenylethyl 155 Me CH 1-(benzyloxycarbonyl)-2-phenylethyl 156 Me CH 1-(phenoxymethyl)-2-phenylethyl 157 Me CH 1-(benzyloxymethyl)-2-phenylethyl 158 Me CH 1-(benzylcarbamoyl)-2-phenylethyl 159 Me CH 1-(N-methylbenzylcarbamoyl)-2-phenylethyl 160 Me CH 1-(phenylcarbamoyl)-2-phenylethyl 161 Me CH 1-(M-methylphenylcarbamoyl)-2-phenylethyl 162 Me CH 1-(N-benzylaminomethyl)-2-phenylethyl 163 Me CH 1-(N-benzyl-N-methylaminomethyl)-2-phenylethyl 164 Me CH 1-(anilinomethyl)-2-phenylethyl 165 Me CH 1-(N-methylanilinomethyl)-2-phenylethyl 166 Me CH 1-(N-methylaminomethyl)-2-phenylethyl 167 Me CH 1-(N-ethylaminomethyl)-2-phenylethyl 168 Me CH 1-(N-isobutylaminomethyl)-2-phenylethyl 169 Me CH 1-(N-cyclopropylmethylaminomethyl)-2-phenyl- ethyl 170 Me CH 1-(aminomethyl)-2-phenylethyl 171 Me CH 1-benzyl-2-(2-pyridylmethylamino)ethyl 172 Me CH 1-benzyl-2-(3-pyridylmethylamino)ethyl 173 Me CH 1-benzyl-2-(4-pyridylmethylamino)ethyl 174 Me CH 2-phenyl-1-(2-pyridylmethylcarbamoyl)ethyl 175 Me CH 2-phenyl-1-(3-pyridylmethylcarbamoyl)ethyl 176 Me CH 2-phenyl-1-(4-pyridylmethylcarbamoyl)ethyl 177 Me CH 2-hydroxy-2-phenylethyl 178 Me CH benzoylmethyl 179 Me CH 1-(benzyloxycarbonyl)-2-(3-indolyl)ethyl 180 Me CH 1-(benzyloxycarbonyl)-2-cyclohexylethyl 181 Me CH 1-(phenoxymethyl)-2-(3-indolyl)ethyl 182 Me CH 2-(2-methoxyphenoxy)ethyl 183 Me CH 1-(benzylcarbarnoyl)-2-cyclohexylethyl 184 Me CH 1-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 185 Me CH 1-(phenylcarbamoyl)-2-cyclohexylethyl 186 Me CH 1-(N-methylphenylcarbamoyl)-2-cyclohexylethyl 187 Me CH 1-(benzyloxycarbonyl)-2-(3-pyridyl)ethyl 188 Me CH 1-(benzylaminomethyl)-2-(3-pyridyl)ethyl 189 Me CH 1-(benzylcarbamoyl)-2-(4-pyridyl)ethyl 190 Me CH 1-(4-pyridylmethylcarbamoyl)-2-(4-fluoro- phenyl) ethyl 191 Me CH 1-(benzylcarbamoyl)-2-(7-aza-3-indolyl)ethyl 192 Me CH 1-(benzyloxymethyl)-2-(2-indolyl)ethyl 193 Me CH 1-(N-benzyl-N-methylaxninomethyl)-2-(3- pyridyl)ethyl 194 Me CH 1-(N-methylbenzylcarbamoyl)-2-(3-pyridyl)ethyl 195 Me CH 2-hydroxy-2-(4-dimethylaminophenyl)ethyl 196 Me CH 2-hydroxy-2-(2-quinolyl)ethyl 197 Me CH 2-hydroxy-2-(3-quinolyl)ethyl 198 Me CH 2-hydroxy-2-(4-quinolyl)ethyl 199 Me CH 2-hydroxy-2-(3,5-difluorophenyl)ethyl 200 Me CH 1-carboxy-2-cyclohexylethyl 201 Me CH 2-hydroxy-2-(6-quinolyl)ethyl 202 Me CH 2-(benzylamino)-2-phenylethyl 203 Me CH 2-amino-2-(2-naphthyl)propyl 204 Me CH 2-(phenylamino)ethyl 205 Me CH diphenylmethyl 206 Me CH 2,2-diphenylethyl 207 Me CH 2-phenyl-2-(2-pyridyl)ethyl 208 Me CH 2-phenyl-2-(3-pyridyl)ethyl 209 Me CH 2-phenyl-2-(4-pyridyl)ethyl 210 Me CH 2-phenoxy-2-phenylethyl 211 Me CH 2-(benzyloxy)-2-phenylethyl 212 Et CH 1-phenyl-3-pyrrolidinyl 213 Et CH 1-(2-fluorophenyl)-3-pyrrolidinyl 214 Et CH 1-(3-fluorophenyl)-3-pyrrolidinyl 215 Et CH 1-(4-fluorophenyl)-3-pyrrolidinyl 216 Et CH 1-(2-chlorophenyl)-3-pyrrolidinyl 217 Et CH 1-(3-chlorophenyl)-3-pyrrolidinyl 218 Et CH 1-(4-chlorophenyl)-3-pyrrolidinyl 219 Et CH 1-(2-methylphenyl)-3-pyrrolidinyl 220 Et CH 1-(3-methylphenyl)-3-pyrrolidinyl 221 Et CH 1-(4-methylphenyl)-3-pyrrolidinyl 222 Et CH 1-(2-methoxyphenyl)-3-pyrrolidinyl 223 Et CH 1-(3-methoxyphenyl)-3-pyrrolidinyl 224 Et CH 1-(4-methoxyphenyl)-3-pyrrolidinyl 225 Et CH 1-(2-trifluoromethylphenyl)-3-pyrrolidinyl 226 Et CH 1-(3-trifluoromethylphenyl)-3-pyrrolidinyl 227 Et CH 1-(4-trifluoromethylphenyl)-3-pyrrolidinyl 228 Et CH 1-(3,5-difluorophenyl)-3-pyrrolidinyl 229 Et CH 1-(2-difluoromethoxyphenyl)-3-pyrrolidinyl 230 Et CH 1-(3-difluoromethoxyphenyl)-3-pyrrolidinyl 231 Et CH 1-(4-difluoromethoxyphenyl)-3-pyrrolidinyl 232 Et CH 1-(2-pyridyl)-3-pyrrolidinyl 233 Et CH 1-(3-pyridyl)-3-pyrrolidinyl 234 Et CH 1-(4-pyridyl)-3-pyrrolidinyl 235 Et CH 1-(2-pyrimidinyl)-3-pyrrolidinyl 236 Et CH 5-oxo-1-phenyl-3-pyrrolidinyl 237 Et CH 1-phenyl-3-piperidyl 238 Et CH 1-(2-fluorophenyl)-3-piperidyl 239 Et CH 1-(3-fluorophenyl)-3-piperidyl 240 Et CH 1-(4-fluorophenyl)-3-piperidyl 241 Et CH 1-(2-chlorophenyl)-3-piperidyl 242 Et CH 1-(3-chlorophenyl)-3-piperidyl 243 Et CH 1-(4-chlorophenyl)-3-piperidyl 244 Et CH 1-(2-methylphenyl)-3-piperidyl 245 Et CH 1-(3-methylphenyl)-3-piperidyl 246 Et CH 1-(4-methylphenyl)-3-piperidyl 247 Et CH 1-(2-methoxyphenyl)-3-piperidyl 248 Et CH 1-(3-methoxyphenyl)-3-piperidyl 249 Et CH 1-(4-methoxyphenyl)-3-piperidyl 250 Et CH 1-(2-trifluoromethylphenyl)-3-piperidyl 251 Et CH 1-(3-trifluoromethylphenyl)-3-piperidyl 252 Et CH 1-(4-trifluoromethylphenyl)-3-piperidyl 253 Et CH 1-(3,5-difluorophenyl)-3-piperidyl 254 Et CH 1-(2-difluoromethoxyphenyl)-3-piperidyl 255 Et CH 1-(3-difluoromethoxyphenyl)-3-piperidyl 256 Et CH 1-(4-difluoromethoxyphenyl)-3-piperidyl 257 Et CH 1-(2-pyridyl)-3-piperidyl 258 Et CH 1-(3-pyridyl)-3-piperidyl 259 Et CH 1-(4-pyridyl)-3-piperidyl 260 Et CH 1-phenyl-4-piperidyl 261 Et CH 1-(2-fluorophenyl)-4-piperidyl 262 Et CH 1-(3-fluorophenyl)-4-piperidyl 263 Et CH 1-(4-fluorophenyl)-4-piperidyl 264 Et CH 1-(2-chloropheny)-4-piperidyl 265 Et CH 1-(3-chloropheny)-4-piperidyl 266 Et CH 1-(4-chloropheny)-4-piperidyl 267 Et CH 1-(2-methylpheny)-4-piperidyl 268 Et CH 1-(3-methylpheny)-4-piperidyl 269 Et CH 1-(4-methylpheny)-4-piperidyl 270 Et CH 1-(2-methoxypheny)-4-piperidyl 271 Et CH 1-(3-methoxypheny)-4-piperidyl 272 Et CH 1-(4-methoxypheny)-4-piperidyl 273 Et CH 1-(2-trifluoromethylpheny)-4-piperidyl 274 Et CH 1-(3-trifluoromethylpheny)-4-piperidyl 275 Et CH 1-(4-trifluoromethylpheny)-4-piperidyl 276 Et CH 1-(3,5-difluorophenyl)-4-piperidyl 277 Et CH 1-(2-difluoromethoxyphenyl)-4-piperidyl 278 Et CH 1-(3-difluoromethoxyphenyl)-4-piperidyl 279 Et CH 1-(4-difluoromethoxyphenyl)-4-piperidyl 280 Et CH 1-(2-pyridyl)-4-piperidyl 281 Et CH 1-(3-pyridyl)-4-piperidyl 282 Et CH 1-(4-pyridyl)-4-piperidyl 283 Et CH 3-hydroxymethyl-1-phenyl-4-piperidyl 284 Et CH 3-methoxycarbonyl-1-phenyl-4-piperidyl 285 Et CH 3-ethoxycarbonyl-1-phenyl-4-piperidyl 286 Et CH 3-isopropoxycarbonyl-1-phenyl-4-piperidyl 287 Et CH 4-phenylcyclohexyl 288 Et CH 4-(2-fluorophenyl)cyclohexyl 289 Et CH 4-(3-fluorophenyl)cyclohexyl 290 Et CH 4-(4-fluorophenyl)cyclohexyl 291 Et CH 4-(2-chlorophenyl)cyclohexyl 292 Et CH 4-(3-chlorophenyl)cyclohexyl 293 Et CH 4-(4-chlorophenyl)cyclohexyl 294 Et CH 4-(2-methylphenyl)cyclohexyl 295 Et CH 4-(3-methylphenyl)cyclohexyl 296 Et CH 4-(4-methylphenyl)cyclohexyl 297 Et CH 4-(2-methoxyphenyl)cyclohexyl 298 Et CH 4-(3-methoxyphenyl)cyclohexyl 299 Et CH 4-(4-methoxyphenyl)cyclohexyl 300 Et CH 4-(2-trifluoromethylphenyl)cyclohexyl 301 Et CH 4-(3-trifluoromethylphenyl)cyclohexyl 302 Et CH 4-(4-trifluoromethylphenyl)cyclohexyl 303 Et CH 4-(3,5-difluorophenyl)cyclohexyl 304 Et CH 4-(3-acetylphenyl)cyclohexyl 305 Et CH 4-(3-cyanophenyl)cyclohexyl 306 Et CH 4-(2-difluoromethoxyphenyl)cyclohexyl 307 Et CH 4-(3-difluoromethoxyphenyl)cyclohexyl 308 Et CH 4-(4-difluoromethoxyphenyl)cyclohexyl 309 Et CH 4-(2-pyridyl)cyclohexyl 310 Et CH 4-(3-pyridyl)cyclohexyl 311 Et CH 4-(4-pyridyl)cyclohexyl 312 Et CH 4-(4-fluoro-3-pyridyl)cyclohexyl 313 Et CH 4-(3-quinolyl)cyclohexyl 314 Et CH 4-(3-fluorophenyl)-4-hydroxycyclohexyl 315 Et CH 3-phenylcyclohexyl 316 Et CH 3-phenylcyclopentyl 317 Et CH 6-phenyl-3-tetrahydropyranyl 318 Et CH 6-(3-fluorophenyl)-3-tetrahydropyranyl 319 Et CH 2-phenylcyclopropyl 320 Et CH 2-(2-pyridyl)cyclopropyl 321 Et CH 2-(3-pyridyl)cyclopropyl 322 Et CH 2-(4-pyridyl)cyclopropyl 323 Et CH 2-(3-fluorophenyl)cyclopropyl 324 Et CH 2-indanyl 325 Et CH 2-tetrahydronaphthyl 326 Et CH 6-methoxy-2-tetrahydronaphthyl 327 Et CH benzyl 328 Et CH phenethyl 329 Et CH 3-phenylpropyl 330 Et CH 4-phenylbutyl 331 Et CH 2-methoxyphenethyl 332 Et CH 3-methoxyphenethyl 333 Et CH 4-methoxyphenethyl 334 Et CH 4-fluorophenethyl 335 Et CH 4-bromophenethyl 336 Et CH 4-chlorophenethyl 337 Et CH 3-trifluoromethylphenethyl 338 Et CH 3,4-dimethoxyphenethyl 339 Et CH 3-propoxyphenethyl 340 Et CH 3,5-difluorophenethyl 341 Et CH 4-dimethylaminophenethyl 342 Et CH 3-difluoromethoxyphenethyl 343 Et CH 2-methylphenethyl 344 Et CH 4-acetylphenethyl 345 Et CH 4-dimethylamino-2-methoxyphenethyl 346 Et CH cyclohexylethyl 347 Et CH 2-(2-pyridyl)ethyl 348 Et CH 2-(3-pyridyl)ethyl 349 Et CH 2-(4-pyridyl)ethyl 350 Et CH 2-(2-quinolyl)ethyl 351 Et CH 2-(3-quinolyl)ethyl 352 Et CH 2-(4-quinolyl)ethyl 353 Et CH 2-(6-quinolyl)ethyl 354 Et CH 2-(2-indolyl)ethyl 355 Et CH 2-(3-indolyl)ethyl 356 Et CH 2-(7-aza-3-indolyl)ethyl 357 Et CH 2-(benzimidazolyl)ethyl 358 Et CH 2-(benzoxazolyl)ethyl 359 Et CH 2-(benzothiazolyl)ethyl 360 Et CH 2-(1-naphthyl)ethyl 361 Et CH 2-(2-naphthyl)ethyl 362 Et CH 1-(hydroxymethyl)-2-phenylethyl 363 Et CH 1-(methoxycarbonyl)-2-phenylethyl 364 Et CH 1-(ethoxycarbonyl)-2-phenylethyl 365 Et CH 1-carboxy-2-phenylethyl 366 Et CH 1-(benzyloxycarbonyl)-2-phenylethyl 367 Et CH 1-(phenoxymethyl)-2-phenylethyl 368 Et CH 1-(benzyloxymethyl)-2-phenylethyl 369 Et CH 1-(benzylcarbamoyl)-2-phenylethyl 370 Et CH 1-(N-methylbenzylcarbamoyl)-2-phenylethyl 371 Et CH 1-(phenylcarbamoyl)-2-phenylethyl 372 Et CH 1-(N-methylphenylcarbamoyl)-2-phenylethyl 373 Et CH 1-(N-benzylaminomethyl)-2-phenylethyl 374 Et CH 1-(N-benzyl-N-methylaminomethyl)-2-phenylethyl 375 Et CH 1-(anilinomethyl)-2-phenylethyl 376 Et CH 1-(N-methylanilinomethyl)-2-phenylethyl 377 Et CH 1-(N-methylaminomethyl)-2-phenylethyl 378 Et CH 1-(N-ethylaxninomethyl)-2-phenylethyl 379 Et CH 1-(N-isobutylaminomethyl)-2-phenylethyl 380 Et CH 1-(N-cyclopropylmethylaminomethyl)-2-phenyl- ethyl 381 Et CH 1-(aminomethyl)-2-phenylethyl 382 Et CH 1-benzyl-2-(2-pyridylmethylamino)ethyl 383 Et CH 1-benzyl-2-(3-pyridylmethylamino)ethyl 384 Et CH 1-benzyl-2-(4-pyridylmethylamino)ethyl 385 Et CH 2-phenyl-1-(2-pyridylmethylcarbamoyl)ethyl 386 Et CH 2-phenyl-1-(3-pyridylmethylcarbamoyl)ethyl 387 Et CH 2-phenyl-1-(4-pyridylmethylcarbamoyl)ethyl 388 Et CH 2-hydroxy-2-phenylethyl 389 Et CH benzoylmethyl 390 Et CH 1-(benzyloxycarbonyl)-2-(3-indolyl)ethyl 391 Et CH 1-(benzyloxycarbonyl)-2-cyclohexylethyl 392 Et CH 1-(phenoxymethyl)-2-(3-indolyl)ethyl 393 Et CH 2-(2-methoxyphenoxyy)ethyl 394 Et CH 1-(benzylcarbamoyl)-2-cyclohexylethyl 395 Et CH 1-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 396 Et CH 1-(phenylcarbarnoyl)-2-cyclohexylethyl 397 Et CH 1-(N-methylphenylcarbamoyl)-2-cyclohexylethyl 398 Et CH 1-(benzyloxycarbonyl)-2-(3-pyridyl)ethyl 399 Et CH 1-(benzylaxninomethyl)-2-(3-pyridyl)ethyl 400 Et CH 1-(benzylcarbamoyl)-2-(4-pyridyl)ethyl 401 Et CH 1-(4-pyridylmethylcarbanioyl)-2-(4-fluoro- phenyl)ethyl 402 Et CH 1-(benzylcarbamoyl)-2-(7-aza-3-indolyl)ethyl 403 Et CH 1-(benzyloxymethyl)-2-(2-indolyl)ethyl 404 Et CH 1-(N-benzyl-N-methylaminomethyl)-2-(3- pyridyl)ethyl 405 Et CH 1-(N-methylbenzylcarbamoyl)-2-(3-pyridyl)ethyl 406 Et CH 2-hydroxy-2-(4-dimethylaminophenyl)ethyl 407 Et CH 2-hydroxy-2-(2-quinolyl)ethyl 408 Et CH 2-hydroxy-2-(3-quinolyl)ethyl 409 Et CH 2-hydroxy-2-(4-quinolyl)ethyl 410 Et CH 2-hydroxy-2-(3,5-difluorophenyl)ethyl 411 Et CH 1-carboxy-2-cyclohexylethyl 412 Et CH 2-hydroxy-2-(6-quinolyl)ethyl 413 Et CH 2-(benzylamino)-2-phenylethyl 414 Et CH 2-amino-2-(2-naphthyl)propyl 415 Et CH 2-(phenylamino)ethyl 416 Et CH diphenylmethyl 417 Et CH 2,2-diphenylethyl 418 Et CH 2-phenyl-2-(2-pyridyl)ethyl 419 Et CH 2-phenyl-2-(3-pyridyl)ethyl 420 Et CH 2-phenyl-2-(4-pyridyl)ethyl 421 Et CH 2-phenoxy-2-phenylethyl 422 Et CH 2-(benzyloxy)-2-phenylethyl 423 Me N 1-phenyl-3-pyrrolidinyl 424 Me N 1-(2-fluorophenyl)-3-pyrrolidinyl 425 Me N 1-(3-fluorophenyl)-3-pyrrolidinyl 426 Me N 1-(4-fluorophenyl)-3-pyrrolidinyl 427 Me N 1-(2-chlorophenyl)-3-pyrrolidinyl 428 Me N 1-(3-chlorophenyl)-3-pyrrolidinyl 429 Me N 1-(4-chlorophenyl)-3-pyrrolidinyl 430 Me N 1-(2-methylphenyl)-3-pyrrolidinyl 431 Me N 1-(3-methylphenyl)-3-pyrrolidinyl 432 Me N 1-(4-methylphenyl)-3-pyrrolidinyl 433 Me N 1-(2-methoxyphenyl)-3-pyrrolidinyl 434 Me N 1-(3-methoxyphenyl)-3-pyrrolidinyl 435 Me N 1-(4-methoxyphenyl)-3-pyrrolidinyl 436 Me N 1-(2-trifluoromethylphenyl)-3-pyrrolidinyl 437 Me N 1-(3-trifluoromethylphenyl)-3-pyrrolidinyl 438 Me N 1-(4-trifluoromethylphenyl)-3-pyrrolidinyl 439 Me N 1-(3,5-difluorophenyl)-3-pyrrolidinyl 440 Me N 1-(2-difluoromethoxyphenyl)-3-pyrrolidinyl 441 Me N 1-(3-difluoromethoxyphenyl)-3-pyrrolidinyl 442 Me N 1-(4-difluoromethoxyphenyl)-3-pyrrolidinyl 443 Me N 1-(2-pyridyl)-3-pyrrolidinyl 444 Me N 1-(3-pyridyl)-3-pyrrolidinyl 445 Me N 1-(4-pyridyl)-3-pyrrolidinyl 446 Me N 1-(2-pyrimidinyl)-3-pyrrolidinyl 447 Me N 5-oxo-1-phenyl-3-pyrrolidinyl 448 Me N 1-phenyl-3-piperidyl 449 Me N 1-(2-fluorophenyl)-3-piperidyl 450 Me N 1-(3-fluorophenyl)-3-piperidyl 451 Me N 1-(4-fluorophenyl)-3-piperidyl 452 Me N 1-(2-chlorophenyl)-3-piperidyl 453 Me N 1-(3-chlorophenyl)-3-piperidyl 454 Me N 1-(4-chlorophenyl)-3-piperidyl 455 Me N 1-(2-methylphenyl)-3-piperidyl 456 Me N 1-(3-methylphenyl)-3-piperidyl 457 Me N 1-(4-methylphenyl)-3-piperidyl 458 Me N 1-(2-methoxyphenyl)-3-piperidyl 459 Me N 1-(3-methoxyphenyl)-3-piperidyl 460 Me N 1-(4-methoxyphenyl)-3-piperidyl 461 Me N 1-(2-trifluoromethylphenyl)-3-piperidyl 462 Me N 1-(3-trifluoromethylphenyl)-3-piperidyl 463 Me N 1-(4-trifluoromethylphenyl)-3-piperidyl 464 Me N 1-(3,5-difluorophenyl)-3-piperidyl 465 Me N 1-(2-difluoromethoxyphenyl)-3-piperidyl 466 Me N 1-(3-difluoromethoxyphenyl)-3-piperidyl 467 Me N 1-(4-difluoromethoxyphenyl)-3-piperidyl 468 Me N 1-(2-pyridyl)-3-piperidyl 469 Me N 1-(3-pyridyl)-3-piperidyl 470 Me N 1-(4-pyridyl)-3-piperidyl 471 Me N 1-phenyl-4-piperidyl 472 Me N 1-(2-fluorophenyl)-4-piperidyl 473 Me N 1-(3-fluorophenyl)-4-piperidyl 474 Me N 1-(4-fluorophenyl)-4-piperidyl 475 Me N 1-(2-chlorophenyl)-4-piperidyl 476 Me N 1-(3-chlorophenyl)-4-piperidyl 477 Me N 1-(4-chlorophenyl)-4-piperidyl 478 Me N 1-(2-methylphenyl)-4-piperidyl 479 Me N 1-(3-methylphenyl)-4-piperidyl 480 Me N 1-(4-methylphenyl)-4-piperidyl 481 Me N 1-(2-methoxyphenyl)-4-piperidyl 482 Me N 1-(3-methoxyphenyl)-4-piperidyl 483 Me N 1-(4-methoxyphenyl)-4-piperidyl 484 Me N 1-(2-trifluoromethylphenyl)-4-piperidyl 485 Me N 1-(3-trifluoromethylphenyl)-4-piperidyl 486 Me N 1-(4-trifluoromethylphenyl)-4-piperidyl 487 Me N 1-(3,5-difluorophenyl)-4-piperidyl 488 Me N 1-(2-difluoromethoxyphenyl)-4-piperidyl 489 Me N 1-(3-difluoromethoxyphenyl)-4-piperidyl 490 Me N 1-(4-difluoromethoxyphenyl)-4-piperidyl 491 Me N 1-(2-pyridyl)-4-piperidyl 492 Me N 1-(3-pyridyl)-4-piperidyl 493 Me N 1-(4-pyridyl)-4-piperidyl 494 Me N 3-hydroxymethyl-1-phenyl-4-piperidyl 495 Me N 3-methoxycarbonyl-1-phenyl-4-piperidyl 496 Me N 3-ethoxycarbonyl-1-phenyl-4-piperidyl 497 Me N 3-isopropoxycarbonyl-1-phenyl-4-piperidyl 498 Me N 4-phenylcyclohexyl 499 Me N 4-(2-fluorophenyl)cyclohexyl 500 Me N 4-(3-fluorophenyl)cyclohexyl 501 Me N 4-(4-fluorophenyl)cyclohexyl 502 Me N 4-(2-chlorophenyl)cyclohexyl 503 Me N 4-(3-chlorophenyl)cyclohexyl 504 Me N 4-(4-chlorophenyl)cyclohexyl 505 Me N 4-(2-methylphenyl)cyclohexyl 506 Me N 4-(3-methylphenyl)cyclohexyl 507 Me N 4-(4-methylphenyl)cyclohexyl 508 Me N 4-(2-methoxyphenyl)cyclohexyl 509 Me N 4-(3-methoxyphenyl)cyclohexyl 510 Me N 4-(4-methoxyphenyl)cyclohexyl 511 Me N 4-(2-trifluoromethylphenyl)cyclohexyl 512 Me N 4-(3-trifluoromethylphenyl)cyclohexyl 513 Me N 4-(4-trifluoromethylphenyl)cyclohexyl 514 Me N 4-(3,5-difluorophenyl)cyclohexyl 515 Me N 4-(3-acetylphenyl)cyclohexyl 516 Me N 4-(3-cyanophenyl)cyclohexyl 517 Me N 4-(2-difluoromethoxyphenyl)cyclohexyl 518 Me N 4-(3-difluoromethoxyphenyl)cyclohexyl 519 Me N 4-(4-difluoromethoxyphenyl)cyclohexyl 520 Me N 4-(2-pyridyl)cyclohexyl 521 Me N 4-(3-pyridyl)cyclohexyl 522 Me N 4-(4-pyridyl)cyclohexyl 523 Me N 4-(4-fluoro-3-pyridyl)cyclohexyl 524 Me N 4-(3-quinolyl)cyclohexyl 525 Me N 4-(3-fluorophenyl)-4-hydroxycyclohexyl 526 Me N 3-phenylcyclohexyl 527 Me N 3-phenylcyclopentyl 528 Me N 6-phenyl-3-tetrahydropyranyl 529 Me N 6-(3-fluorophenyl)-3-tetrahydropyranyl 530 Me N 2-phenylcyclopropyl 531 Me N 2-(2-pyridyl)cyclopropyl 532 Me N 2-(3-pyridyl)cyclopropyl 533 Me N 2-(4-pyridyl)cyclopropyl 534 Me N 2-(3-fluorophenyl)cyclopropyl 535 Me N 2-indanyl 536 Me N 2-tetrahydronaphthyl 537 Me N 6-methoxy-2-tetrahydronaphthyl 538 Me N benzyl 539 Me N phenethyl 540 Me N 3-phenylpropyl 541 Me N 4-phenylbutyl 542 Me N 2-methoxyphenethyl 543 Me N 3-methoxyphenethyl 544 Me N 4-methoxyphenethyl 545 Me N 4-fluorophenethyl 546 Me N 4-bromophenethyl 547 Me N 4-chlorophenethyl 548 Me N 3-trifluoromethylphenethyl 549 Me N 3,4-dimethoxyphenethyl 550 Me N 3-propoxyphenethyl 551 Me N 3,5-difluorophenethyl 552 Me N 4-dimethylaminophenethyl 553 Me N 3-difluoromethoxyphenethyl 554 Me N 2-methylphenethyl 555 Me N 4-acetylphenethyl 556 Me N 4-dimethylamino-2-methoxyphenethyl 557 Me N cyclohexylethyl 558 Me N 2-(2-pyridyl)ethyl 559 Me N 2-(3-pyridyl)ethyl 560 Me N 2-(4-pyridyl)ethyl 561 Me N 2-(2-quinolyl)ethyl 562 Me N 2-(3-quinolyl)ethyl 563 Me N 2-(4-quinolyl)ethyl 564 Me N 2-(6-quinolyl)ethyl 565 Me N 2-(2-indolyl)ethyl 566 Me N 2-(3-indolyl)ethyl 567 Me N 2-(7-aza-3-indolyl)ethyl 568 Me N 2-(benzimidazolyl)ethyl 569 Me N 2-(benzoxazolyl)ethyl 570 Me N 2-(benzothiazolyl)ethyl 571 Me N 2-(1-naphthyl)ethyl 572 Me N 2-(2-naphthyl)ethyl 573 Me N 1-(hydroxymethyl)-2-phenylethyl 574 Me N 1-(methoxycarbonyl)-2-phenylethyl 575 Me N 1-(ethoxycarbonyl)-2-phenylethyl 576 Me N 1-carboxy-2-phenylethyl 577 Me N 1-(benzyloxycarbonyl)-2-phenylethyl 578 Me N 1-(phenoxymethyl)-2-phenylethyl 579 Me N 1-(benzyloxymethyl)-2-phenylethyl 580 Me N 1-(benzylcarbamoyl)-2-phenylethyl 581 Me N 1-(N-methylbenzylcarbamoyl)-2-phenylethyl 582 Me N 1-(phenylcarbamoyl)-2-phenylethyl 583 Me N 1-(N-methylphenylcarbamoyl)-2-phenylethyl 584 Me N 1-(N-benzylaminomethyl)-2-phenylethyl 585 Me N 1-(N-benzyl-N-methylaminomethyl)-2-phenylethyl 586 Me N 1-(anilinomethyl)-2-phenylethyl 587 Me N 1-(N-methylanilinomethyl)-2-phenylethyl 588 Me N 1-(N-methylaminomethyl)-2-phenylethyl 589 Me N 1-(N-ethylaminomethyl)-2-phenylethyl 590 Me N 1-(N-isobutylaminomethyl)-2-phenylethyl 591 Me N 1-(N-cyclopropylmethylaminomethyl)-2-phenyl- ethyl 592 Me N 1-(aminomethyl)-2-phenylethyl 593 Me N 1-benzyl-2-(2-pyridylmethylamino)ethyl 594 Me N 1-benzyl-2-(3-pyridylmethylamino)ethyl 595 Me N 1-benzyl-2-(4-pyridylmethylamino)ethyl 596 Me N 2-phenyl-1-(2-pyridylmethylcarbamoyl)ethyl 597 Me N 2-phenyl-1-(3-pyridylmethylcarbamoyl)ethyl 598 Me N 2-phenyl-1-(4-pyridylmethylcarbamoyl)ethyl 599 Me N 2-hydroxy-2-phenylethyl 600 Me N benzoylmethyl 601 Me N 1-(benzyloxycarbonyl)-2-(3-indolyl)ethyl 602 Me N 1-(benzyloxycarbonyl)-2-cyclohexylethyl 603 Me N 1-(phenoxymethyl)-2-(3-indolyl)ethyl 604 Me N 2-(2-methoxyphenoxy)ethyl 605 Me N 1-(benzylcarbamoyl)-2-cyclohexylethyl 606 Me N 1-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 607 Me N 1-(phenylcarbamoyl)-2-cyclohexylethyl 608 Me N 1-(N-methylphenylcarbamoyl)-2-cyclohexylethyl 609 Me N 1-(benzyloxycarbonyl)-2-(3-pyridyl)ethyl 610 Me N 1-(benzylaminomethyl)-2-(3-pyridyl)ethyl 611 Me N 1-(benzylcarbamoyl)-2-(4-pyridyl)ethyl 612 Me N 1-(4-pyridylmethylcarbamoyl)-2-(4-fluoro- phenyl) ethyl 613 Me N 1-(benzylcarbamoyl)-2-(7-aza-3-indolyl)ethyl 614 Me N 1-(benzyloxymethyl)-2-(2-indolyl)ethyl 615 Me N 1-(N-benzyl-N-methylaminomethyl)-2-(3- pyridyl)ethyl 616 Me N 1-(N-methylbenzylcarbamoyl)-2-(3-pyridyl)ethyl 617 Me N 2-hydroxy-2-(4-dimethylaminophenyl)ethyl 618 Me N 2-hydroxy-2-(2-quinolyl)ethyl 619 Me N 2-hydroxy-2-(3-quinolyl)ethyl 620 Me N 2-hydroxy-2-(4-quinolyl)ethyl 621 Me N 2-hydroxy-2-(3,5-difluorophenyl)ethyl 622 Me N 1-carboxy-2-cyclohexylethyl 623 Me N 2-hydroxy-2-(6-quinolyl)ethyl 624 Me N 2-(benzylamino)-2-phenylethyl 625 Me N 2-amino-2-(2-naphthyl)propyl 626 Me N 2-(phenylamino)ethyl 627 Me N diphenylmethyl 628 Me N 2,2-diphenylethyl 629 Me N 2-phenyl-2-(2-pyridyl)ethyl 630 Me N 2-phenyl-2-(3-pyridyl)ethyl 631 Me N 2-phenyl-2-(4-pyridyl)ethyl 632 Me N 2-phenoxy-2-phenylethyl 633 Me N 2-(benzyloxy)-2-phenylethyl 634 Et N 1-phenyl-3-pyrrolidinyl 635 Et N 1-(2-fluorophenyl)-3-pyrrolidinyl 636 Et N 1-(3-fluorophenyl)-3-pyrrolidinyl 637 Et N 1-(4-fluorophenyl)-3-pyrrolidinyl 638 Et N 1-(2-chlorophenyl)-3-pyrrolidinyl 639 Et N 1-(3-chlorophenyl)-3-pyrrolidinyl 640 Et N 1-(4-chlorophenyl)-3-pyrrolidinyl 641 Et N 1-(2-methylphenyl)-3-pyrrolidinyl 642 Et N 1-(3-methylphenyl)-3-pyrrolidinyl 643 Et N 1-(4-methylphenyl)-3-pyrrolidinyl 644 Et N 1-(2-methoxyphenyl)-3-pyrrolidinyl 645 Et N 1-(3-methoxyphenyl)-3-pyrrolidinyl 646 Et N 1-(4-methoxyphenyl)-3-pyrrolidinyl 647 Et N 1-(2-trifluoromethylphenyl)-3-pyrrolidinyl 648 Et N 1-(3-trifluoromethylphenyl)-3-pyrrolidinyl 649 Et N 1-(4-trifluoromethylphenyl)-3-pyrrolidinyl 650 Et N 1-(3,5-difluorophenyl)-3-pyrrolidinyl 651 Et N 1-(2-difluoromethoxyphenyl)-3-pyrrolidinyl 652 Et N 1-(3-difluoromethoxyphenyl)-3-pyrrolidinyl 653 Et N 1-(4-difluoromethoxyphenyl)-3-pyrrolidinyl 654 Et N 1-(2-pyridyl)-3-pyrrolidinyl 655 Et N 1-(3-pyridyl)-3-pyrrolidinyl 656 Et N 1-(4-pyridyl)-3-pyrrolidinyl 657 Et N 1-(2-pyrimidinyl)-3-pyrrolidinyl 658 Et N 5-oxo-1-phenyl-3-pyrrolidinyl 659 Et N 1-phenyl-3-piperidyl 660 Et N 1-(2-fluorophenyl)-3-piperidyl 661 Et N 1-(3-fluorophenyl)-3-piperidyl 662 Et N 1-(4-fluorophenyl)-3-piperidyl 663 Et N 1-(2-chlorophenyl)-3-piperidyl 664 Et N 1-(3-chlorophenyl)-3-piperidyl 665 Et N 1-(4-chlorophenyl)-3-piperidyl 666 Et N 1-(2-methylphenyl)-3-piperidyl 667 Et N 1-(3-methylphenyl)-3-piperidyl 668 Et N 1-(4-methylphenyl)-3-piperidyl 669 Et N 1-(2-methoxyphenyl)-3-piperidyl 670 Et N 1-(3-methoxyphenyl)-3-piperidyl 671 Et N 1-(4-methoxyphenyl)-3-piperidyl 672 Et N 1-(2-trifluoromethylphenyl)-3-piperidyl 673 Et N 1-(3-trifluoromethylphenyl)-3-piperidyl 674 Et N 1-(4-trifluoromethylphenyl)-3-piperidyl 675 Et N 1-(3,5-difluorophenyl)-3-piperidyl 676 Et N 1-(2-difluoromethoxyphenyl)-3-piperidyl 677 Et N 1-(3-difluoromethoxyphenyl)-3-piperidyl 678 Et N 1-(4-difluoromethoxyphenyl)-3-piperidyl 679 Et N 1-(2-pyridyl)-3-piperidyl 680 Et N 1-(3-pyridyl)-3-piperidyl 681 Et N 1-(4-pyridyl)-3-piperidyl 682 Et N 1-phenyl-4-piperidyl 683 Et N 1-(2-fluorophenyl)-4-piperidyl 684 Et N 1-(3-fluorophenyl)-4-piperidyl 685 Et N 1-(4-fluorophenyl)-4-piperidyl 686 Et N 1-(2-chlorophenyl)-4-piperidyl 687 Et N 1-(3-chlorophenyl)-4-piperidyl 688 Et N 1-(4-chlorophenyl)-4-piperidyl 689 Et N 1-(2-methylphenyl)-4-piperidyl 690 Et N 1-(3-methylphenyl)-4-piperidyl 691 Et N 1-(4-methylphenyl)-4-piperidyl 692 Et N 1-(2-methoxyphenyl)-4-piperidyl 693 Et N 1-(3-methoxyphenyl)-4-piperidyl 694 Et N 1-(4-methoxyphenyl)-4-piperidyl 695 Et N 1-(2-trifluoromethylphenyl)-4-piperidyl 696 Et N 1-(3-trifluoromethylphenyl)-4-piperidyl 697 Et N 1-(4-trifluoromethylphenyl)-4-piperidyl 698 Et N 1-(3,5-difluorophenyl)-4-piperidyl 699 Et N 1-(2-difluoromethoxyphenyl)-4-piperidyl 700 Et N 1-(3-difluoromethoxyphenyl)-4-piperidyl 701 Et N 1-(4-difluoromethoxyphenyl)-4-piperidyl 702 Et N 1-(2-pyridyl)-4-piperidyl 703 Et N 1-(3-pyridyl)-4-piperidyl 704 Et N 1-(4-pyridyl)-4-piperidyl 705 Et N 3-hydroxymethyl-1-phenyl-4-piperidyl 706 Et N 3-methoxycarbonyl-1-phenyl-4-piperidyl 707 Et N 3-ethoxycarbonyl-1-phenyl-4-piperidyl 708 Et N 3-isopropoxycarbonyl-1-phenyl-4-piperidyl 709 Et N 4-phenylcyclohexyl 710 Et N 4-(2-fluorophenyl)cyclohexyl 711 Et N 4-(3-fluorophenyl)cyclohexyl 712 Et N 4-(4-fluorophenyl)cyclohexyl 713 Et N 4-(2-chlorophenyl)cyclohexyl 714 Et N 4-(3-chlorophenyl)cyclohexyl 715 Et N 4-(4-chlorophenyl)cyclohexyl 716 Et N 4-(2-methylphenyl)cyclohexyl 717 Et N 4-(3-methylphenyl)cyclohexyl 718 Et N 4-(4-methylphenyl)cyclohexyl 719 Et N 4-(2-methoxyphenyl)cyclohexyl 720 Et N 4-(3-methoxyphenyl)cyclohexyl 721 Et N 4-(4-methoxyphenyl)cyclohexyl 722 Et N 4-(2-trifluoromethylphenyl)cyclohexyl 723 Et N 4-(3-trifluoromethylphenyl)cyclohexyl 724 Et N 4-(4-trifluoromethylphenyl)cyclohexyl 725 Et N 4-(3,5-difluorophenyl)cyclohexyl 726 Et N 4-(3-acetylphenyl)cyclohexyl 727 Et N 4-(3-cyanophenyl)cyclohexyl 728 Et N 4-(2-difluoromethoxyphenyl)cyclohexyl 729 Et N 4-(3-difluoromethoxyphenyl)cyclohexyl 730 Et N 4-(4-difluoromethoxyphenyl)cyclohexyl 731 Et N 4-(2-pyridyl)cyclohexyl 732 Et N 4-(3-pyridyl)cyclohexyl 733 Et N 4-(4-pyridyl)cyclohexyl 734 Et N 4-(4-fluoro-3-pyridyl)cyclohexyl 735 Et N 4-(3-quinolyl)cyclohexyl 736 Et N 4-(3-fluorophenyl)-4-hydroxycyclohexyl 737 Et N 3-phenylcyclohexyl 738 Et N 3-phenylcyclopentyl 739 Et N 6-phenyl-3-tetrahydropyranyl 740 Et N 6-(3-fluorophenyl)-3-tetrahydropyranyl 741 Et N 2-phenylcyclopropyl 742 Et N 2-(2-pyridyl)cyclopropyl 743 Et N 2-(3-pyridyl)cyclopropyl 744 Et N 2-(4-pyridyl)cyclopropyl 745 Et N 2-(3-fluorophenyl)cyclopropyl 746 Et N 2-indanyl 747 Et N 2-tetrahydronaphthyl 748 Et N 6-methoxy-2-tetrahydronaphthyl 749 Et N benzyl 750 Et N phenethyl 751 Et N 3-phenylpropyl 752 Et N 4-phenylbutyl 753 Et N 2-methoxyphenethyl 754 Et N 3-methoxyphenethyl 755 Et N 4-methoxyphenethyl 756 Et N 4-fluorophenethyl 757 Et N 4-bromophenethyl 758 Et N 4-chlorophenethyl 759 Et N 3-trifluoromethylphenethyl 760 Et N 3,4-dimethoxyphenethyl 761 Et N 3-propoxyphenethyl 762 Et N 3,5-difluorophenethyl 763 Et N 4-dimethylaminophenethyl 764 Et N 3-difluoromethoxyphenethyl 765 Et N 2-methylphenethyl 766 Et N 4-acetylphenethyl 767 Et N 4-dimethylamino-2-methoxyphenethyl 768 Et N cyclohexylethyl 769 Et N 2-(2-pyridyl)ethyl 770 Et N 2-(3-pyridyl)ethyl 771 Et N 2-(4-pyridyl)ethyl 772 Et N 2-(2-quinolyl)ethyl 773 Et N 2-(3-quinolyl)ethyl 774 Et N 2-(4-quinolyl)ethyl 775 Et N 2-(6-quinolyl)ethyl 776 Et N 2-(2-indolyl)ethyl 777 Et N 2-(3-indolyl)ethyl 778 Et N 2-(7-aza-3-indolyl)ethyl 779 Et N 2-(benzimidazolyl)ethyl 780 Et N 2-(benzoxazolyl)ethyl 781 Et N 2-(benzothiazolyl)ethyl 782 Et N 2-(1-naphthyl)ethyl 783 Et N 2-(2-naphthyl)ethyl 784 Et N 1-(hydroxymethyl)-2-phenylethyl 785 Et N 1-(methoxycarbonyl)-2-phenylethyl 786 Et N 1-(ethoxycarbonyl)-2-phenylethyl 787 Et N 1-carboxy-2-phenylethyl 788 Et N 1-(benzyloxycarbonyl)-2-phenylethyl 789 Et N 1-(phenoxymethyl)-2-phenylethyl 790 Et N 1-(benzyloxymethyl)-2-phenylethyl 791 Et N 1-(benzylcarbamoyl)-2-phenylethyl 792 Et N 1-(N-methylbenzylcarbamoyl)-2-phenylethyl 793 Et N 1-(phenylcarbamoyl)-2-phenylethyl 794 Et N 1-(N-methylphenylcarbamoyl)-2-phenylethyl 795 Et N 1-(N-benzylaminomethyl)-2-phenylethyl 796 Et N 1-(N-benzyl-N-methylaminomethyl)-2-phenylethyl 797 Et N 1-(anilinomethyl)-2-phenylethyl 798 Et N 1-(N-methylanilinomethyl)-2-phenylethyl 799 Et N 1-(N-methylaminomethyl)-2-phenylethyl 800 Et N 1-(N-ethylaminomethyl)-2-phenylethyl 801 Et N 1-(N-isobutylaminomethyl)-2-phenylethyl 802 Et N 1-(N-cyclopropylmethylaminomethyl)-2-phenyl- ethyl 803 Et N 1-(aminomethyl)-2-phenylethyl 804 Et N 1-benzyl-2-(2-pyridylmethylamino)ethyl 805 Et N 1-benzyl-2-(3-pyridylmethylamino)ethyl 806 Et N 1-benzyl-2-(4-pyridylmethylamino)ethyl 807 Et N 2-phenyl-1-(2-pyridylmethylcarbamoyl)ethyl 808 Et N 2-phenyl-1-(3-pyridylmethylcarbamoyl)ethyl 809 Et N 2-phenyl-1-(4-pyridylmethylcarbamoyl)ethyl 810 Et N 2-hydroxy-2-phenylethyl 811 Et N benzoylmethyl 812 Et N 1-(benzyloxycarbonyl)-2-(3-indolyl)ethyl 813 Et N 1-(benzyloxycarbonyl)-2-cyclohexylethyl 814 Et N 1-(phenoxymethyl)-2-(3-indolyl)ethyl 815 Et N 2-(2-methoxyphenoxy)ethyl 816 Et N 1-(benzylcarbamoyl)-2-cyclohexylethyl 817 Et N 1-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 818 Et N 1-(phenylcarbamoyl)-2-cyclohexylethyl 819 Et N 1-(N-methylphenylcarbamoyl)-2-cyclohexylethyl 820 Et N 1-(benzyloxycarbonyl)-2-(3-pyridyl)ethyl 821 Et N 1-(benzylaminomethyl)-2-(3-pyridyl)ethyl 822 Et N 1-(benzylcarbamoyl)-2-(4-pyridyl)ethyl 823 Et N 1-(4-pyridylmethylcarbamoyl)-2-(4-fluoro- phenyl)ethyl 824 Et N 1-(benzylcarbamoyl)-2-(7-aza-3-indolyl)ethyl 825 Et N 1-(benzyloxymethyl)-2-(2-indolyl)ethyl 826 Et N 1-(N-benzyl-N-methylaminomethyl)-2-(3- pyridyl)ethyl 827 Et N 1-(N-methylbenzylcarbamoyl)-2-(3-pyridyl)ethyl 828 Et N 2-hydroxy-2-(4-dimethylaminophenyl)ethyl 829 Et N 2-hydroxy-2-(2-quinolyl)ethyl 830 Et N 2-hydroxy-2-(3-quinolyl)ethyl 831 Et N 2-hydroxy-2-(4-quinolyl)ethyl 832 Et N 2-hydroxy-2-(3,5-difluorophenyl)ethyl 833 Et N 1-carboxy-2-cyclohexylethyl 834 Et N 2-hydroxy-2-(6-quinolyl)ethyl 835 Et N 2-(benzylamino)-2-phenylethyl 836 Et N 2-amino-2-(2-naphthyl)propyl 837 Et N 2-(phenylamino)ethyl 838 Et N diphenylmethyl 839 Et N 2,2-diphenylethyl 840 Et N 2-phenyl-2-(2-pyridyl)ethyl 841 Et N 2-phenyl-2-(3-pyridyl)ethyl 842 Et N 2-phenyl-2-(4-pyridyl)ethyl 843 Et N 2-phenoxy-2-phenylethyl 844 Et N 2-(benzyloxy)-2-phenylethyl

[0155] TABLE 2

No. A—Ar¹—R⁰ 845 1-phenyl-3-pyrrolidinyl 846 1-(2-fluorophenyl)-3-pyrrolidinyl 847 1-(3-fluorophenyl)-3-pyrrolidinyl 848 1-(4-fluorophenyl)-3-pyrrolidinyl 849 1-(2-chlorophenyl)-3-pyrrolidinyl 850 1-(3-chlorophenyl)-3-pyrrolidinyl 851 1-(4-chlorophenyl)-3-pyrrolidinyl 852 1-(2-methylphenyl)-3-pyrrolidinyl 853 1-(3-methylphenyl)-3-pyrrolidinyl 854 1-(4-methylphenyl)-3-pyrrolidinyl 855 1-(2-methoxphenyl)-3-pyrrolidinyl 856 1-(3-methylphenyl)-3-pyrrolidinyl 857 1-(4-methylphenyl)-3-pyrrolidinyl 858 1-(2-trifluoromethylphenyl)-3-pyrrolidinyl 859 1-(3-trifluoromethylphenyl)-3-pyrrolidinyl 860 1-(4-trifluoromethylphenyl)-3-pyrrolidinyl 861 1-(3,5-difluorophenyl)-3-pyrrolidinyl 862 1-(2-difluoromethoxyphenyl)-3-pyrrolidinyl 863 1-(3-difluoromethoxyphenyl)-3-pyrrolidinyl 864 1-(4-difluoromethoxyphenyl)-3-pyrrolidinyl 865 1-(2-pyridyl)-3-pyrrolidinyl 866 1-(3-pyridyl)-3-pyrrolidinyl 867 1-(4-pyridyl)-3-pyrrolidinyl 868 1-(2-pyrimidinyl)-3-pyrrolidinyl 869 5-oxo-1-phenyl-3-pyrrolidinyl 870 1-phenyl-3-piperidyl 871 1-(2-fluorophenyl)-3-piperidyl 872 1-(3-fluorophenyl)-3-piperidyl 873 1-(4-fluorophenyl)-3-piperidyl 874 1-(2-chlorophenyl)-3-piperidyl 875 1-(3-chlorophenyl)-3-piperidyl 876 1-(4-chlorophenyl)-3-piperidyl 877 1-(2-methylphenyl)-3-piperidyl 878 1-(3-methylphenyl)-3-piperidyl 879 1-(4-methylphenyl)-3-piperidyl 880 1-(2-methoxyphenyl)-3-piperidyl 881 1-(3-methoxyphenyl)-3-piperidyl 882 1-(4-methoxyphenyl)-3-piperidyl 883 1-(2-trifluoromethylphenyl)-3-piperidyl 884 1-(3-trifluoromethylphenyl)-3-piperidyl 885 1-(4-trifluoromethylphenyl)-3-piperidyl 886 1-(3,5-difluorophenyl)-3-piperidyl 887 1-(2-difluoromethoxyphenyl)-3-piperidyl 888 1-(3-difluoromethoxyphenyl)-3-piperidyl 889 1-(4-difluoromethoxyphenyl)-3-piperidyl 890 1-(2-pyridyl)-3-piperidyl 891 1-(3-pyridyl)-3-piperidyl 892 1-(4-pyridyl)-3-piperidyl 893 1-phenyl-4-piperidyl 894 1-(2-fluorophenyl)-4-piperidyl 895 1-(3-fluorophenyl)-4-piperidyl 896 1-(4-fluorophenyl)-4-piperidyl 897 1-(2-chlorophenyl)-4-piperidyl 898 1-(3-chlorophenyl)-4-piperidyl 899 1-(4-chlorophenyl)-4-piperidyl 900 1-(2-methylphenyl)-4-piperidyl 901 1-(3-methylphenyl)-4-piperidyl 902 1-(4-methylphenyl)-4-piperidyl 903 1-(2-methoxyphenyl)-4-piperidyl 904 1-(3-methoxyphenyl)-4-piperidyl 905 1-(4-methoxyphenyl)-4-piperidyl 906 1-(2-trifluoromethylphenyl)-4-piperidyl 907 1-(3-trifluoromethylphenyl)-4-piperidyl 908 1-(4-trifluoromethylphenyl)-4-piperidyl 909 1-(3,5-difluorophenyl)-4-piperidyl 910 1-(2-difluoromethoxyphenyl)-4-piperidyl 911 1-(3-difluoromethoxyphenyl)-4-piperidyl 912 1-(4-difluoromethoxyphenyl)-4-piperidyl 913 1-(2-pyridyl)-4-piperidyl 914 1-(3-pyridyl)-4-piperidyl 915 1-(4-pyridyl)-4-piperidyl 916 3-hydroxymethyl-1-phenyl-4-piperidyl 917 3-methoxycarbonyl-1-phenyl-4-piperidyl 918 3-ethoxycarbonyl-1-phenyl-4-piperidyl 919 3-isopropoxycarbonyl-1-phenyl-4-piperidyl 920 4-phenylcyclohexyl 921 4-(2-fluorophenyl)cyclohexyl 922 4-(3-fluorophenyl)cyclohexyl 923 4-(4-fluorophenyl)cyclohexyl 924 4-(2-chlorophenyl)cyclohexyl 925 4-(3-chlorophenyl)cyclohexyl 926 4-(4-chlorophenyl)cyclohexyl 927 4-(2-methylphenyl)cyclohexyl 928 4-(3-methylphenyl)cyclohexyl 929 4-(4-methylphenyl)cyclohexyl 930 4-(2-methoxyphenyl)cyclohexyl 931 4-(3-methoxyphenyl)cyclohexyl 932 4-(4-methoxyphenyl)cyclohexyl 933 4-(2-trifluoromethylphenyl)cyclohexyl 934 4-(3-trifluoromethylphenyl)cyclohexyl 935 4-(4-trifluoromethylphenyl)cyclohexyl 936 4-(3,5-difluorophenyl)cyclohexyl 937 4-(3-acetylphenyl)cyclohexyl 938 4-(3-cyanophenyl)cyclohexyl 939 4-(2-difluoromethoxyphenyl)cyclohexyl 940 4-(3-difluoromethoxyphenyl)cyclohexyl 941 4-(4-difluoromethoxyphenyl)cyclohexyl 942 4-(2-pyridyl)cyclohexyl 943 4-(3-pyridyl)cyclohexyl 944 4-(4-pyridyl)cyclohexyl 945 4-(4-fluoro-3-pyridyl)cyclohexyl 946 4-(3-quinolyl)cyclohexyl 947 4-(3-fluorophenyl)-4-hydroxycyclohexyl 948 3-phenylcyclohexyl 949 3-phenylcyclopentyl 950 6-phenyl-3-tetrahydropyranyl 951 6-(3-fluorophenyl)-3-tetrahydropyranyl 952 2-phenylcyclopropyl 953 2-(2-pyridyl)cyclopropyl 954 2-(3-pyridyl)cyclopropyl 955 2-(4-pyridyl)cyclopropyl 956 2-(3-fluorophenyl)cyclopropyl 957 2-indanyl 958 2-tetrahydronaphthyl 959 6-methoxy-2-tetrahydronaphthyl 960 benzyl 961 phenethyl 962 3-phenylpropyl 963 4-phenylbutyl 964 2-methoxyphenethyl 965 3-methoxyphenethyl 966 4-methoxyphenethyl 967 4-fluorophenethyl 968 4-bromophenethyl 969 4-chlorophenethyl 970 3-trifluoromethylphenethyl 971 3,4-dimethoxyphenethyl 972 3-propoxyphenethyl 973 3,5-difluorophenethyl 974 4-dimethylaminophenethyl 975 3-difluoromethoxyphenethyl 976 2-methylphenethyl 977 4-acetylphenethyl 978 4-dimethylamino-2-methoxyphenethyl 979 cyclohexylethyl 980 2-(2-pyridyl)ethyl 981 2-(3-pyridyl)ethyl 982 2-(4-pyridyl)ethyl 983 2-(2-quinolyl)ethyl 984 2-(3-quinolyl)ethyl 985 2-(4-quinolyl)ethyl 986 2-(6-quinolyl)ethyl 987 2-(2-indolyl)ethyl 988 2-(3-indolyl)ethyl 989 2-(7-aza-3-indolyl)ethyl 990 2-(benzimidazolyl)ethyl 991 2-(benzoxazolyl)ethyl 992 2-(benzothiazolyl)ethyl 993 2-(1-naphthyl)ethyl 994 2-(2-naphthyl)ethyl 995 1-(hydroxymethyl)-2-phenylethyl 996 1-(methoxycarbonyl)-2-phenylethyl 997 1-(ethoxycarbonyl)-2-phenylethyl 998 1-carboxy-2-phenylethyl 999 1-(benzyloxycarbonyl)-2-phenylethyl 1000 1-(phenoxymethyl)-2-phenylethyl 1001 1-(benzyloxymethyl)-2-phenylethyl 1002 1-(benzylcarbamoyl)-2-phenylethyl 1003 1-(N-methylbenzylcarbamoyl)-2-phenylethyl 1004 1-(phenylcarbamoyl)-2-phenylethyl 1005 1-(N-methylphenylcarbamoyl)-2-phenylethyl 1006 1-(N-benzylaminomethyl)-2-phenylethyl 1007 1-(N-benzyl-N-methylaminomethyl)-2-phenylethyl 1008 1-(anilinomethyl)-2-phenylethyl 1009 1-(N-methylanilinomethyl)-2-phenylethyl 1010 1-(N-methylaminomethyl)-2-phenylethyl 1011 1-(N-ethylaminomethyl)-2-phenylethyl 1012 1-(N-isobutylaminomethyl)-2-phenylethyl 1013 1-(N-cyclopropylmethylaminomethyl)-2-phenylethyl 1014 1-(aminomethyl)-2-phenylethyl 1015 1-benzyl-2-(2-pyridylmethylamino)ethyl 1016 1-benzyl-2-(3-pyridylmethylamino)ethyl 1017 1-benzyl-2-(4-pyridylmethylamino)ethyl 1018 2-phenyl-1-(2-pyridylmethylcarbarnoyl)ethyl 1019 2-phenyl-1-(3-pyridylmethylcarbamoyl)ethyl 1020 2-phenyl-1-(4-pyridylmethylcarbamoyl)ethyl 1021 2-hydroxy-2-phenylethyl 1022 benzoylmethyl 1023 1-(benzyloxycarbonyl)-2-(3-indolyl)ethyl 1024 1-(benzyloxycarbonyl)-2-cyclohexylethyl 1025 1-(phenoxymethyl)-2-(3-indolyl)ethyl 1026 2-(2-methoxyphenoxy)ethyl 1027 1-(benzylcarbamoyl)-2-cyclohexylethyl 1028 1-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 1029 1-(phenylcarbamoyl)-2-cyclohexylethyl 1030 1-(N-methylphenylcarbamoyl)-2-cyclohexylethyl 1031 1-(benzyloxycarbonyl)-2-(3-pyridyl)ethyl 1032 1-(benzylaminomethyl)-2-(3-pyridyl)ethyl 1033 1-(benzylcarbamoyl)-2-(4-pyridyl)ethyl 1034 1-(4-pyridylmethylcarbamoyl)-2-(4-fluorophenyl)ethyl 1035 1-(benzylcarbanioyl)-2-(7-aza-3-indolyl)ethyl 1036 1-(benzyloxymethyl)-2-(2-indolyl)ethyl 1037 1-(N-benzyl-N-methylaminomethyl)-2-(3-pyridyl)ethyl 1038 1-(N-methylbenzylcarbamoyl)-2-(3-pyridyl)ethyl 1039 2-hydroxy-2-(4-dimethylaminophenyl)ethyl 1040 2-hydroxy-2-(2-quinolyl)ethyl 1041 2-hydroxy-2-(3-quinolyl)ethyl 1042 2-hydroxy-2-(4-quinolyl)ethyl 1043 2-hydroxy-2-(3,5-difluorophenyl)ethyl 1044 1-carboxy-2-cyclohexylethyl 1045 2-hydroxy-2-(6-quinolyl)ethyl 1046 2-(benzylamino)-2-phenylethyl 1047 2-amino-2-(2-naphthyl)propyl 1048 2-(phenylamino)ethyl 1049 diphenylmethyl 1050 2,2-diphenylethyl 1051 2-phenyl-2-(2-pyridyl)ethyl 1052 2-phenyl-2-(3-pyridyl)ethyl 1053 2-phenyl-2-(4-pyridyl)ethyl 1054 2-phenoxy-2-phenylethyl 1055 2-(benzyloxy)-2-phenylethyl

[0156] TABLE 3

No. T U V W Z A—Ar¹—R⁰ 1056 CH CH CH CH CH 1-phenyl-3-pyrrolidinyl 1057 CH CH CH CH CH 1-(2-fluorophenyl)-3- pyrrolidinyl 1058 CH CH CH CH CH 1-(3-fluorophenyl)-3- pyrrolidinyl 1059 CH CH CH CH CH 1-(4-fluorophenyl)-3- pyrrolidinyl 1060 CH CH CH CH CH 1-(2-chlorophenyl)-3- pyrrolidinyl 1061 CH CH CH CH CH 1-(3-chlorophenyl)-3- pyrrolidinyl 1062 CH CH CH CH CH 1-(4-chlorophenyl)-3- pyrrolidinyl 1063 CH CH CH CH CH 1-(2-methylphenyl)-3- pyrrolidinyl 1064 CH CH CH CH CH 1-(3-methylphenyl)-3- pyrrolidinyl 1065 CH CH CH CH CH 1-(4-methylphenyl)-3- pyrrolidinyl 1066 CH CH CH CH CH 1-(2-methoxyyphenyl)-3- pyrrolidinyl 1067 CH CH CH CH CH 1-(3-methoxyyphenyl)-3- pyrrolidinyl 1068 CH CH CH CH CH 1-(4-methoxyyphenyl)-3- pyrrolidinyl 1069 CH CH CH CH CH 1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 1070 CH CH CH CH CH 1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 1071 CH CH CH CH CH 1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 1072 CH CH CH CH CH 1-(3,5-difluorophenyl)-3- pyrrolidinyl 1073 CH CH CH CH CH 1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 1074 CH CH CH CH CH 1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 1075 CH CH CH CH CH 1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 1076 CH CH CH CH CH 1-(2-pyridyl)-3-pyrrolidinyl 1077 CH CH CH CH CH 1-(3-pyridyl)-3-pyrrolidinyl 1078 CH CH CH CH CH 1-(4-pyridyl)-3-pyrrolidinyl 1079 CH CH CH CH CH 1-(2-pyrimidinyl)-3-pyrrolidinyl 1080 CH CH CH CH CH 5-oxo-1-phenyl-3-pyrrolidinyl 1081 CH CH CH CH CH 1-phenyl-3-piperidyl 1082 CH CH CH CH CH 1-(2-fluorophenyl)-3-piperidyl 1083 CH CH CH CH CH 1-(3-fluorophenyl)-3-piperidyl 1084 CH CH CH CH CH 1-(4-fluorophenyl)-3-piperidyl 1085 CH CH CH CH CH 1-(2-chlorophenyl)-3-piperidyl 1086 CH CH CH CH CH 1-(3-chlorophenyl)-3-piperidyl 1087 CH CH CH CH CH 1-(4-chlorophenyl)-3-piperidyl 1088 CH CH CH CH CH 1-(2-methylphenyl)-3-piperidyl 1089 CH CH CH CH CH 1-(3-methylphenyl)-3-piperidyl 1090 CH CH CH CH CH 1-(4-methylphenyl)-3-piperidyl 1091 CH CH CH CH CH 1-(2-methoxyphenyl)-3-piperidyl 1092 CH CH CH CH CH 1-(3-methoxyphenyl)-3-piperidyl 1093 CH CH CH CH CH 1-(4-methoxyphenyl)-3-piperidyl 1094 CH CH CH CH CH 1-(2-trifluoromethylphenyl)-3- piperidyl 1095 CH CH CH CH CH 1-(3-trifluoromethylphenyl)-3- piperidyl 1096 CH CH CH CH CH 1-(4-trifluoromethylphenyl)-3- piperidyl 1097 CH CH CH CH CH 1-(3,5-difluorophenyl)-3-piperidyl 1098 CH CH CH CH CH 1-(2-difluoromethoxyphenyl)-3- piperidyl 1099 CH CH CH CH CH 1-(3-difluoromethoxyphenyl)-3- piperidyl 1100 CH CH CH CH CH 1-(4-difluorornethoxyphenyl)-3- piperidyl 1101 CH CH CH CH CH 1-(2-pyridyl)-3-piperidyl 1102 CH CH CH CH CH 1-(3-pyridyl)-3-piperidyl 1103 CH CH CH CH CH 1-(4-pyridyl)-3-piperidyl 1104 CH CH CH CH CH 1-phenyl-4-piperidyl 1105 CH CH CH CH CH 1-(2-fluorophenyl)-4-piperidyl 1106 CH CH CH CH CH 1-(3-fluorophenyl)-4-piperidyl 1107 CH CH CH CH CH 1-(4-fluorophenyl)-4-piperidyl 1108 CH CH CH CH CH 1-(2-chlorophenyl)-4-piperidyl 1109 CH CH CH CH CH 1-(3-chlorophenyl)-4-piperidyl 1110 CH CH CH CH CH 1-(4-chlorophenyl)-4-piperidyl 1111 CH CH CH CH CH 1-(2-methylphenyl)-4-piperidyl 1112 CH CH CH CH CH 1-(3-methylphenyl)-4-piperidyl 1113 CH CH CH CH CH 1-(4-methylphenyl)-4-piperidyl 1114 CH CH CH CH CH 1-(2-methoxyphenyl)-4-piperidyl 1115 CH CH CH CH CH 1-(3-methoxyphenyl)-4-piperidyl 1116 CH CH CH CH CH 1-(4-methoxyphenyl)-4-piperidyl 1117 CH CH CH CH CH 1-(2-trifluoromethylphenyl)-4- piperidyl 1118 CH CH CH CH CH 1-(3-trifluoromethylphenyl)-4- piperidyl 1119 CH CH CH CH CH 1-(4-trifluoromethylphenyl)-4- piperidyl 1120 CH CH CH CH CH 1-(3,5-difluorophenyl)-4-piperidyl 1121 CH CH CH CH CH 1-(2-difluoromethoxyphenyl)-4- piperidyl 1122 CH CH CH CH CH 1-(3-difluoromethoxyphenyl)-4- piperidyl 1123 CH CH CH CH CH 1-(4-difluoromethoxyphenyl)-4- piperidyl 1124 CH CH CH CH CH 1-(2-pyridyl)-4-piperidyl 1125 CH CH CH CH CH 1-(3-pyridyl)-4-piperidyl 1126 CH CH CH CH CH 1-(4-pyridyl)-4-piperidyl 1127 CH CH CH CH CH 3-hydroxymethyl-1-phenyl-4- piperidyl 1128 CH CH CH CH CH 3-methoxycarbonyl-1-phenyl-4- piperidyl 1129 CH CH CH CH CH 3-ethoxycarbonyl-1-phenyl-4- piperidyl 1130 CH CH CH CH CH 3-isopropoxycarbonyl-1-phenyl-4- piperidyl 1131 CH CH CH CH CH 4-phenylcyclohexyl 1132 CH CH CH CH CH 4-(2-fluorophenyl)cyclohexyl 1133 CH CH CH CH CH 4-(3-fluorophenyl)cyclohexyl 1134 CH CH CH CH CH 4-(4-fluorophenyl)cyclohexyl 1135 CH CH CH CH CH 4-(2-chlorophenyl)cyclohexyl 1136 CH CH CH CH CH 4-(3-chlorophenyl)cyclohexyl 1137 CH CH CH CH CH 4-(4-chlorophenyl)cyclohexyl 1138 CH CH CH CH CH 4-(2-methylphenyl)cyclohexyl 1139 CH CH CH CH CH 4-(3-methylphenyl)cyclohexyl 1140 CH CH CH CH CH 4-(4-methylphenyl)cyclohexyl 1141 CH CH CH CH CH 4-(2-methoxyphenyl)cyclohexyl 1142 CH CH CH CH CH 4-(3-methoxyphenyl)cyclohexyl 1143 CH CH CH CH CH 4-(4-methoxyphenyl)cyclohexyl 1144 CH CH CH CH CH 4-(2-trifluoromethylphenyl)cyclo- hexyl 1145 CH CH CH CH CH 4-(3-trifluoromethylphenyl)cyclo- hexyl 1146 CH CH CH CH CH 4-(4-trifluoromethylphenyl)cyclo- hexyl 1147 CH CH CH CH CH 4-(3,5-difluorophenyl)cyclohexyl 1148 CH CH CH CH CH 4-(3-acetylphenyl)cyclohexyl 1149 CH CH CH CH CH 4-(3-cyanophenyl)cyclohexyl 1150 CH CH CH CH CH 4-(2-difluoromethoxyphenyl)cyclo- hexyl 1151 CH CH CH CH CH 4-(3-difluoromethoxyphenyl)cyclo- hexyl 1152 CH CH CH CH CH 4-(4-difluoromethoxyphenyl)cyclo- hexyl 1153 CH CH CH CH CH 4-(2-pyridyl)cyclohexyl 1154 CH CH CH CH CH 4-(3-pyridyl)cyclohexyl 1155 CH CH CH CH CH 4-(4-pyridyl)cyclohexyl 1156 CH CH CH CH CH 4-(4-fluoro-3-pyridyl)cyclohexyl 1157 CH CH CH CH CH 4-(3-quinolyl)cyclohexyl 1158 CH CH CH CH CH 4-(3-fluorophenyl)-4-hydroxy- cyclohexyl 1159 CH CH CH CH CH 3-phenylcyclohexyl 1160 CH CH CH CH CH 3-phenylcyclopentyl 1161 CH CH CH CH CH 6-phenyl-3-tetrhydropyranyl 1162 CH CH CH CH CH 6-(3-fluorophenyl)-3-tetrhydro- pyranyl 1163 CH CH CH CH CH 2-phenylcyclopropyl 1164 CH CH CH CH CH 2-(2-pyridyl)cyclopropyl 1165 CH CH CH CH CH 2-(3-pyridyl)cyclopropyl 1166 CH CH CH CH CH 2-(4-pyridyl)cyclopropyl 1167 CH CH CH CH CH 2-(3-fluorophenyl)cyclopropyl 1168 CH CH CH CH CH 2-indanyl 1169 CH CH CH CH CH 2-tetrahydronaphthyl 1170 CH CH CH CH CH 6-methoxy-2-tetrahydronaphthyl 1171 CH CH CH CH CH benzyl 1172 CH CH CH CH CH phenethyl 1173 CH CH CH CH CH 3-phenylpropyl 1174 CH CH CH CH CH 4-phenylbutyl 1175 CH CH CH CH CH 2-methoxyphenethyl 1176 CH CH CH CH CH 3-methoxyphenethyl 1177 CH CH CH CH CH 4-methoxyphenethyl 1178 CH CH CH CH CH 4-fluorophenethyl 1179 CH CH CH CH CH 4-bromophenethyl 1180 CH CH CH CH CH 4-chlorophenethyl 1181 CH CH CH CH CH 3-trifluoromethylphenethyl 1182 CH CH CH CH CH 3,4-dimethoxyphenethyl 1183 CH CH CH CH CH 3-propoxyphenethyl 1184 CH CH CH CH CH 3,5-difluorophenethyl 1185 CH CH CH CH CH 4-dimethylaminophenethyl 1186 CH CH CH CH CH 3-difluoromethoxyphenethyl 1187 CH CH CH CH CH 2-methylphenethyl 1188 CH CH CH CH CH 4-acetylphenethyl 1189 CH CH CH CH CH 4-dimethylamino-2-methoxyphenethyl 1190 CH CH CH CH CH cyclohexylethyl 1191 CH CH CH CH CH 2-(2-pyridyl)ethyl 1192 CH CH CH CH CH 2-(3-pyridyl)ethyl 1193 CH CH CH CH CH 2-(4-pyridyl)ethyl 1194 CH CH CH CH CH 2-(2-quinolyl)ethyl 1195 CH CH CH CH CH 2-(3-quinolyl)ethyl 1196 CH CH CH CH CH 2-(4-quinolyl)ethyl 1197 CH CH CH CH CH 2-(6-quinolyl)ethyl 1198 CH CH CH CH CH 2-(2-indolyl)ethyl 1199 CH CH CH CH CH 2-(3-indolyl)ethyl 1200 CH CH CH CH CH 2-(7-aza-3-indolyl)ethyl 1201 CH CH CH CH CH 2-(benzimidazolyl)ethyl 1202 CH CH CH CH CH 2-(benzoxazolyl)ethyl 1203 CH CH CH CH CH 2-(benzothiazolyl)ethyl 1204 CH CH CH CH CH 2-(1-naphthyl)ethyl 1205 CH CH CH CH CH 2-(2-naphthyl)ethyl 1206 CH CH CH CH CH 1-(hydroxymethyl)-2-phenylethyl 1207 CH CH CH CH CH 1-(methoxycarbonyl)-2-phenylethyl 1208 CH CH CH CH CH 1-(ethoxycarbonyl)-2-phenylethyl 1209 CH CH CH CH CH 1-carboxy-2-phenylethyl 1210 CH CH CH CH CH 1-(benzyloxycarbonyl)-2-phenyl- ethyl 1211 CH CH CH CH CH 1-(phenoxymethyl)-2-phenylethyl 1212 CH CH CH CH CH 1-(benzyloxymethyl)-2-phenylethyl 1213 CH CH CH CH CH 1-(benzylcarbamoyl)-2-phenylethyl 1214 CH CH CH CH CH 1-(N-methylbenzylcarbamoyl)-2- phenylethyl 1215 CH CH CH CH CH 1-(phenylcarbamoyl)-2-phenylethyl 1216 CH CH CH CH CH 1-(N-methylphenylcarbamoyl)-2- phenylethyl 1217 CH CH CH CH CH 1-(N-benzylaminomethyl)-2-phenyl- ethyl 1218 CH CH CH CH CH 1-(N-benzyl-N-methylaminomethyl)- 2-phenylethyl 1219 CH CH CH CH CH 1-(anilinomethyl)-2-phenylethyl 1220 CH CH CH CH CH 1-(N-methylanilinomethyl)-2- phenylethyl 1221 CH CH CH CH CH 1-(N-methylaminomethyl)-2- phenylethyl 1222 CH CH CH CH CH 1-(N-ethylaminomethyl)-2- phenylethyl 1223 CH CH CH CH CH 1-(N-isobutylaminomethyl)-2- phenylethyl 1224 CH CH CH CH CH 1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 1225 CH CH CH CH CH 1-(aminomethyl)-2-phenylethyl 1226 CH CH CH CH CH 1-benzyl-2-(2-pyridylmethyl- amino)ethyl 1227 CH CH CH CH CH 1-benzyl-2-(3-pyridylmethyl- amino)ethyl 1228 CH CH CH CH CH 1-benzyl-2-(4-pyridylmethyl- amino)ethyl 1229 CH CH CH CH CH 2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 1230 CH CH CH CH CH 2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 1231 CH CH CH CH CH 2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 1232 CH CH CH CH CH 2-hydroxy-2-phenylethyl 1233 CH CH CH CH CH benzoylmethyl 1234 CH CH CH CH CH 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 1235 CH CH CH CH CH 1-(benzyloxycarbonyl)-2-cyclo- hexylethyl 1236 CH CH CH CH CH 1-(phenoxymethyl)-2-(3- indolyl)ethyl 1237 CH CH CH CH CH 2-(2-methoxyphenoxy)ethyl 1238 CH CH CH CH CH 1-(benzylcarbamoyl)-2-cyclohexyl- ethyl 1239 CH CH CH CH CH 1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 1240 CH CH CH CH CH 1-(phenylcarbamoyl)-2-cyclohexyl- ethyl 1241 CH CH CH CH CH 1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 1242 CH CH CH CH CH 1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 1243 CH CH CH CH CH 1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 1244 CH CH CH CH CH 1-(benzylcarbamoyl)-2-(4- pyridyl)ethyl 1245 CH CH CH CH CH 1-(4-pyridylmethylcarbamoyl)-2-(4- fluorophenyl)ethyl 1246 CH CH CH CH CH 1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 1247 CH CH CH CH CH 1-(benzyloxymethyl)-2-(2- indolyl)ethyl 1248 CH CH CH CH CH 1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 1249 CH CH CH CH CH 1-(N-methylbenzylcarbamoyl)-2- (3-pyridyl)ethyl 1250 CH CH CH CH CH 2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 1251 CH CH CH CH CH 2-hydroxy-2-(2-quinolyl)ethyl 1252 CH CH CH CH CH 2-hydroxy-2-(3-quinolyl)ethyl 1253 CH CH CH CH CH 2-hydroxy-2-(4-quinolyl)ethyl 1254 CH CH CH CH CH 2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 1255 CH CH CH CH CH 1-carboxy-2-cyclohexylethyl 1256 CH CH CH CH CH 2-hydroxy-2-(6-quinolyl)ethyl 1257 CH CH CH CH CH 2-(benzylamino)-2-phenylethyl 1258 CH CH CH CH CH 2-amino-2-(2-naphthyl)propyl 1259 CH CH CH CH CH 2-(phenylamino)ethyl 1260 CH CH CH CH CH diphenylmethyl 1261 CH CH CH CH CH 2,2-diphenylethyl 1262 CH CH CH CH CH 2-phenyl-2-(2-pyridyl)ethyl 1263 CH CH CH CH CH 2-phenyl-2-(3-pyridyl)ethyl 1264 CH CH CH CH CH 2-phenyl-2-(4-pyridyl)ethyl 1265 CH CH CH CH CH 2-phenoxy-2-phenylethyl 1266 CH CH CH CH CH 2-(benzyloxy)-2-phenylethyl 1267 CH CH CH CH N 1-phenyl-3-pyrrolidinyl 1268 CH CH CH. CH N 1-(2-fluorophenyl)-3-pyrrolidinyl 1269 CH CH CH CH N 1-(3-fluorophenyl)-3-pyrrolidinyl 1270 CH CH CH CH N 1-(4-fluorophenyl)-3-pyrrolidinyl 1271 CH CH CH CH N 1-(2-chlorophenyl)-3-pyrrolidinyl 1272 CH CH CH CH N 1-(3-chlorophenyl)-3-pyrrolidinyl 1273 CH CH CH CH N 1-(4-chlorophenyl)-3-pyrrolidinyl 1274 CH CH CH CH N 1-(2-methylphenyl)-3-pyrrolidinyl 1275 CH CH CH CH N 1-(3-methylphenyl)-3-pyrrolidinyl 1276 CH CH CH CH N 1-(4-methylphenyl)-3-pyrrolidinyl 1277 CH CH CH CH N 1-(2-methoxyphenyl)-3-pyrrolidinyl 1278 CH CH CH CH N 1-(3-methoxyphenyl)-3-pyrrolidinyl 1279 CH CH CH CH N 1-(4-methoxyphenyl)-3-pyrrolidinyl 1280 CH CH CH CH N 1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 1281 CH CH CH CH N 1-(3-trifluromethylphenyl)-3- pyrrolidinyl 1282 CH CH CH CH N 1-(4-trifluromethylphenyl)-3- pyrrolidinyl 1283 CH CH CH CH N 1-(3,5-diflurophenyl)-3- pyrrolidinyl 1284 CH CH CH CH N 1-(2-difluromethoxyphenyl)-3- pyrrolidinyl 1285 CH CH CH CH N 1-(3-difluromethoxyphenyl)-3- pyrrolidinyl 1286 CH CH CH CH N 1-(4-difluromethoxyphenyl)-3- pyrrolidinyl 1287 CH CH CH CH N 1-(2-pyridyl)-3-pyrrolidinyl 1288 CH CH CH CH N 1-(3-pyridyl)-3-pyrrolidinyl 1289 CH CH CH CH N 1-(4-pyridyl)-3-pyrrolidinyl 1290 CH CH CH CH N 1-(2-pyrimidinyl)-3-pyrrolidinyl 1291 CH CH CH CH N 5-oxo-1-phenyl-3-pyrrolidinyl 1292 CH CH CH CH N 1-phenyl-3-piperidyl 1293 CH CH CH CH N 1-(2-fluorophenyl)-3-piperidyl 1294 CH CH CH CH N 1-(3-fluorophenyl)-3-piperidyl 1295 CH CH CH CH N 1-(4-fluorophenyl)-3-piperidyl 1296 CH CH CH CH N 1-(2-chlorophenyl)-3-piperidyl 1297 CH CH CH CH N 1-(3-chlorophenyl)-3-piperidyl 1298 CH CH CH CH N 1-(4-chlorophenyl)-3-piperidyl 1299 CH CH CH CH N 1-(2-methylphenyl)-3-piperidyl 1300 CH CH CH CH N 1-(3-methylphenyl)-3-piperidyl 1301 CH CH CH CH N 1-(4-methylphenyl)-3-piperidyl 1302 CH CH CH CH N 1-(2-methoxyphenyl)-3-piperidyl 1303 CH CH CH CH N 1-(3-methoxyphenyl)-3-piperidyl 1304 CH CH CH CH N 1-(4-methoxyphenyl)-3-piperidyl 1305 CH CH CH CH N 1-(2-trifluoromethylphenyl)-3- piperidyl 1306 CH CH CH CH N 1-(3-trifluoromethylphenyl)-3- piperidyl 1307 CH CH CH CH N 1-(4-trifluoromethylphenyl)-3- piperidyl 1308 CH CH CH CH N 1-(3,5-difluorophenyl)-3-piperidyl 1309 CH CH CH CH N 1-(2-difluoromethoxyphenyl)-3- piperidyl 1310 CH CH CH CH N 1-(3-difluoromethoxyphenyl)-3- piperidyl 1311 CH CH CH CH N 1-(4-difluoromethoxyphenyl)-3- piperidyl 1312 CH CH CH CH N 1-(2-pyridyl)-3-piperidyl 1313 CH CH CH CH N 1-(3-pyridyl)-3-piperidyl 1314 CH CH CH CH N 1-(4-pyridyl)-3-piperidyl 1315 CH CH CH CH N 1-phenyl-4-piperidyl 1316 CH CH CH CH N 1-(2-fluorophenyl)-4-piperidyl 1317 CH CH CH CH N 1-(3-fluorophenyl)-4-piperidyl 1318 CH CH CH CH N 1-(4-fluorophenyl)-4-piperidyl 1319 CH CH CH CH N 1-(2-chlorophenyl)-4-piperidyl 1320 CH CH CH CH N 1-(3-chlorophenyl)-4-piperidyl 1321 CH CH CH CH N 1-(4-chlorophenylj-4-piperidyl 1322 CH CH CH CH N 1-(2-methylphenyl)-4-piperidyl 1323 CH CH CH CH N 1-(3-methylphenyl)-4-piperidyl 1324 CH CH CH CH N 1-(4-methylphenyl)-4-piperidyl 1325 CH CH CH CH N 1-(2-methoxyphenyl)-4-piperidyl 1326 CH CH CH CH N 1-(3-methoxyphenyl)-4-piperidyl 1327 CH CH CH CH N 1-(4-methoxyphenyl)-4-piperidyl 1328 CH CH CH CH N 1-(2-trifluoromethylphenyl)-4- piperidyl 1329 CH CH CH CH N 1-(3-trifluoromethylphenyl)-4- piperidyl 1330 CH CH CH CH N 1-(4-trifluoromethylphenyl)-4- piperidyl 1331 CH CH CH CH N 1-(3,5-difluorophenyl)-4- piperidyl 1332 CH CH CH CH N 1-(2-difluoromethoxyphenyl)-4- piperidyl 1333 CH CH CH CH N 1-(3-difluoromethoxyphenyl)-4- piperidyl 1334 CH CH CH CH N 1-(4-difluoromethoxyphenyl)-4- piperidyl 1335 CH CH CH CH N 1-(2-pyridyl)-4-piperidyl 1336 CH CH CH CH N 1-(3-pyridyl)-4-piperidyl 1337 CH CH CH CH N 1-(4-pyridyl)-4-piperidyl 1338 CH CH CH CH N 3-hydroxymethyl-1-phenyl-4- piperidyl 1339 CH CH CH CH N 3-methoxycarbonyl-1-phenyl-4- piperidyl 1340 CH CH CH CH N 3-ethoxycarbonyl-1-phenyl-4- piperidyl 1341 CH CH CH CH N 3-isopropoxycarbonyl-1-phenyl-4- piperidyl 1342 CH CH CH CH N 4-phenylcyclohexyl 1343 CH CH CH CH N 4-(2-fluorophenyl)cyclohexyl 1344 CH CH CH CH N 4-(3-fluorophenyl)cyclohexyl 1345 CH CH CH CH N 4-(4-fluorophenyl)cyclohexyl 1346 CH CH CH CH N 4-(2-chlorophenyl)cyclohexyl 1347 CH CH CH CH N 4-(3-chlorophenyl)cyclohexyl 1348 CH CH CH CH N 4-(4-chlorophenyl)cyclohexyl 1349 CH CH CH CH N 4-(2-methylphenyl)cyclohexyl 1350 CH CH CH CH N 4-(3-methylphenyl)cyclohexyl 1351 CH CH CH CH N 4-(4-methylphenyl)cyclohexyl 1352 CH CH CH CH N 4-(2-methoxyphenyl)cyclohexyl 1353 CH CH CH CH N 4-(3-methoxyphenyl)cyclohexyl 1354 CH CH CH CH N 4-(4-methoxyphenyl)cyclohexyl 1355 CH CH CH CH N 4-(2-trifluoromethylphenyl)cyclo- hexyl 1356 CH CH CH CH N 4-(3-trifluoromethylphenyl)cyclo- hexyl 1357 CH CH CH CH N 4-(4-trifluoromethylphenyl)cyclo- hexyl 1358 CH CH CH CH N 4-(3,5-difluorophenyl)cyclohexyl 1359 CH CH CH CH N 4-(3-acetylphenyl)cyclohexyl 1360 CH CH CH CH N 4-(3-cyanophenyl)cyclohexyl 1361 CH CH CH CH N 4-(2-difluoromethoxyphenyl)cyclo- hexyl 1362 CH CH CH CH N 4-(3-difluoromethoxyphenyl)cyclo- hexyl 1363 CH CH CH CH N 4-(4-difluoromethoxyphenyl)cyclo- hexyl 1364 CH CH CH CH N 4-(2-pyridyl)cyclohexyl 1365 CH CH CH CH N 4-(3-pyridyl)cyclohexyl 1366 CH CH CH CH N 4-(4-pyridyl)cyclohexyl 1367 CH CH CH CH N 4-(4-fluoro-3-pyridyl)cyclohexyl 1368 CH CH CH CH N 4-(3-quinolyl)cyclohexyl 1369 CH CH CH CH N 4-(3-fluorophenyl)-4-hydroxy- cyclohexyl 1370 CH CH CH CH N 3-phenylcyclohexyl 1371 CH CH CH CH N 3-phenylcyclopentyl 1372 CH CH CH CH N 6-phenyl-3-tetrahydropyranyl 1373 CH CH CH CH N 6-(3-fluorophenyl)-3-tetrahydro- pyranyl 1374 CH CH CH CH N 2-phenylcyclopropyl 1375 CH CH CH CH N 2-(2-pyridyl)cyclopropyl 1376 CH CH CH CH N 2-(3-pyridyl)cyclopropyl 1377 CH CH CH CH N 2-(4-pyridyl)cyclopropyl 1378 CH CH CH CH N 2-(3-fluorophenyl)cyclopropyl 1379 CH CH CH CH N 2-indanyl 1380 CH CH CH CH N 2-tetrahydronaphthyl 1381 CH CH CH CH N 6-methoxy-2-tetrahydronaphthyl 1382 CH CH CH CH N benzyl 1383 CH CH CH CH N phenethyl 1384 CH CH CH CH N 3-phenylpropyl 1385 CH CH CH CH N 4-phenylbutyl 1386 CH CH CH CH N 2-methoxyphenethyl 1387 CH CH CH CH N 3-methoxyphenethyl 1388 CH CH CH CH N 4-methoxyphenethyl 1389 CH CH CH CH N 4-fluorophenethyl 1390 CH CH CH CH N 4-bromophenethyl 1391 CH CH CH CH N 4-chlorophenethyl 1392 CH CH CH CH N 3-trifluoromethylphenethyl 1393 CH CH CH CH N 3,4-dimethoxyphenethyl 1394 CH CH CH CH N 3-propoxyphenethyl 1395 CH CH CH CH N 3,5-difluorophenethyl 1396 CH CH CH CH N 4-dimethylaminophenethyl 1397 CH CH CH CH N 3-difluoromethoxyphenethyl 1398 CH CH CH CH N 2-methylphenethyl 1399 CH CH CH CH N 4-acetylphenethyl 1400 CH CH CH CH N 4-dimethylaxnino-2-methoxy- phenethyl 1401 CH CH CH CH N cyclohexylethyl 1402 CH CH CH CH N 2-(2-pyridyl)ethyl 1403 CH CH CH CH N 2-(3-pyridyl)ethyl 1404 CH CH CH CH N 2-(4-pyridyl)ethyl 1405 CH CH CH CH N 2-(2-quinolyl)ethyl 1406 CH CH CH CH N 2-(3-quinolyl)ethyl 1407 CH CH CH CH N 2-(4-quinolyl)ethyl 1408 CH CH CH CH N 2-(6-quinolyl)ethyl 1409 CH CH CH CH N 2-(2-indolyl)ethyl 1410 CH CH CH CH N 2-(3-indolyl)ethyl 1411 CH CH CH CH N 2-(7-aza-3-indolyl)ethyl 1412 CH CH CH CH N 2-(benzimidazolyl)ethyl 1413 CH CH CH CH N 2-(benzoxazolyl)ethyl 1414 CH CH CH CH N 2-(benzothiazolyl)ethyl 1415 CH CH CH CH N 2-(1-naphthyl)ethyl 1416 CH CH CH CH N 2-(2-naphthyl)ethyl 1417 CH CH CH CH N 1-(hydroxymethyl)-2-phenylethyl 1418 CH CH CH CH N 1-(methoxycarbonyl)-2-phenyl- ethyl 1419 CH CH CH CH N 1-(ethoxycarbonyl)-2-phenylethyl 1420 CH CH CH CH N 1-carboxy-2-phenylethyl 1421 CH CH CH CH N 1-(benzyloxycarbonyl)-2-phenyl- ethyl 1422 CH CH CH CH N 1-(phenoxymethyl)-2-phenylethyl 1423 CH CH CH CH N 1-(benzyloxymethyl)-2-phenylethyl 1424 CH CH CH CH N 1-(benzylcarbamoyl)-2-phenylethyl 1425 CH CH CH CH N 1-(N-methylbenzylcarbamoyl)-2- phenylethyl 1426 CH CH CH CH N 1-(phenylcarbamoyl)-2-phenylethyl 1427 CH CH CH CH N 1-(N-methylphenylcarbamoyl)-2- phenylethyl 1428 CH CH CH CH N 1-(N-benzylaminomethyl)-2- phenylethyl 1429 CH CH CH CH N 1-(N-benzyl-N-methylamino- methyl)-2-phenylethyl 1430 CH CH CH CH N 1-(anilinomethyl)-2-phenylethyl 1431 CH CH CH CH N 1-(N-methylanilinomethyl)-2- phenylethyl 1432 CH CH CH CH N 1-(N-methylaminomethyl)-2- phenylethyl 1433 CH CH CH CH N 1-(N-ethylaminomethyl)-2- phenylethyl 1434 CH CH CH CH N 1-(N-isobutylaminomethyl)-2- phenylethyl 1435 CH CH CH CH N 1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 1436 CH CH CH CH N 1-(aminomethyl)-2-phenylethyl 1437 CH CH CH CH N 1-benzyl-2-(2-pyridylmethyl- amino)ethyl 1438 CH CH CH CH N 1-benzyl-2-(3-pyridylmethyl- amino)ethyl 1439 CH CH CH CH N 1-benzyl-2-(4-pyridylmethyl- amino)ethyl 1440 CH CH CH CH N 2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 1441 CH CH CH CH N 2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 1442 CH CH CH CH N 2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 1443 CH CH CH CH N 2-hydroxy-2-phenylethyl 1444 CH CH CH CH N benzoylmethyl 1445 CH CH CH CH N 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 1446 CH CH CH CH N 1-(benzyloxycarbonyl)-2- cyclohexylethyl 1447 CH CH CH CH N 1-(phenoxymethyl)-2-(3- indolyl)ethyl 1448 CH CH CH CH N 2-(2-methoxyphenoxy)ethyl 1449 CH CH CH CH N 1-(benzylcarbamoyl)-2-cyclohexyl- ethyl 1450 CH CH CH CH N 1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 1451 CH CH CH CH N 1-(phenylcarbamoyl)-2-cyclohexyl- ethyl 1452 CH CH CH CH N 1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 1453 CH CH CH CH N 1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 1454 CH CH CH CH N 1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 1455 CH CH CH CH N 1-(benzylcarbamoyl)-2- (4-pyridyl)ethyl 1456 CH CH CH CH N 1-(4-pyridylmethylcarbamoyl)-2- (4-fluorophenyl)ethyl 1457 CH CH CH CH N 1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 1458 CH CH CH CH N 1-(benzyloxymethyl)-2-(2- indolyl)ethyl 1459 CH CH CH CH N 1-(N-benzyl-N-methylaminomethyl)-2- (3-pyridyl)ethyl 1460 CH CH CH CH N 1-(N-methylbenzylcarbamoyl)-2- (3-pyridyl)ethyl 1461 CH CH CH CH N 2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 1462 CH CH CH CH N 2-hydroxy-2-(2-quinolyl)ethyl 1463 CH CH CH CH N 2-hydroxy-2-(3-quinolyl)ethyl 1464 CH CH CH CH N 2-hydroxy-2-(4-quinolyl)ethyl 1465 CH CH CH CH N 2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 1466 CH CH CH CH N 1-carboxy-2-cyclohexylethyl 1467 CH CH CH CH N 2-hydroxy-2-(6-quinolyl)ethyl 1468 CH CH CH CH N 2-(benzylamino)-2-phenylethyl 1469 CH CH CH CH N 2-amino-2-(2-naphthyl)propyl 1470 CH CH CH CH N 2-(phenylamino)ethyl 1471 CH CH CH CH N diphenylmethyl 1472 CH CH CH CH N 2,2-diphenylethyl 1473 CH CH CH CH N 2-phenyl-2-(2-pyridyl)ethyl 1474 CH CH CH CH N 2-phenyl-2-(3-pyridyl)ethyl 1475 CH CH CH CH N 2-phenyl-2-(4-pyridyl)ethyl 1476 CH CH CH CH N 2-phenoxy-2-phenylethyl 1477 CH CH CH CH N 2-(benzyloxy)-2-phenylethyl 1478 N CH CH CH CH 1-phenyl-3-pyrrolidinyl 1479 N CH CH CH CH 1-(2-fluorophenyl)-3-pyrrolidinyl 1480 N CH CH CH CH 1-(3-fluorophenyl)-3-pyrrolidinyl 1481 N CH CH CH CH 1-(4-fluorophenyl)-3-pyrrolidinyl 1482 N CH CH CH CH 1-(2-chlorophenyl)-3-pyrrolidinyl 1483 N CH CH CH CH 1-(3-chlorophenyl)-3-pyrrolidinyl 1484 N CH CH CH CH 1-(4-chlorophenyl)-3-pyrrolidinyl 1485 N CH CH CH CH 1-(2-methylphenyl)-3-pyrrolidinyl 1486 N CH CH CH CH 1-(3-methylphenyl)-3-pyrrolidinyl 1487 N CH CH CH CH 1-(4-methylphenyl)-3-pyrrolidinyl 1488 N CH CH CH CH 1-(2-methoxyphenyl)-3- pyrrolidinyl 1489 N CH CH CH CH 1-(3-methoxyphenyl)-3- pyrrolidinyl 1490 N CH CH CH CH 1-(4-methoxyphenyl)-3- pyrrolidinyl 1491 N CH CH CH CH 1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 1492 N CH CH CH CH 1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 1493 N CH CH CH CH 1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 1494 N CH CH CH CH 1-(3,5-difluorophenyl)-3- pyrrolidinyl 1495 N CH CH CH CH 1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 1496 N CH CH CH CH 1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 1497 N CH CH CH CH 1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 1498 N CH CH CH CH 1-(2-pyridyl)-3-pyrrolidinyl 1499 N CH CH CH CH 1-(3-pyridyl)-3-pyrrolidinyl 1500 N CH CH CH CH 1-(4-pyridyl)-3-pyrrolidinyl 1501 N CH CH CH CH 1-(2-pyrimidinyl)-3-pyrrolidinyl 1502 N CH CH CH CH 5-oxo-1-phenyl-3-pyrrolidinyl 1503 N CH CH CH CH 1-phenyl-3-piperidyl 1504 N CH CH CH CH 1-(2-fluorophenyl)-3-piperidyl 1505 N CH CH CH CH 1-(3-fluorophenyl)-3-piperidyl 1506 N CH CH CH CH 1-(4-fluorophenyl)-3-piperidyl 1507 N CH CH CH CH 1-(2-chlorophenyl)-3-piperidyl 1508 N CH CH CH CH 1-(3-chlorophenyl)-3-piperidyl 1509 N CH CH CH CH 1-(4-chlorophenyl)-3-piperidyl 1510 N CH CH CH CH 1-(2-methylphenyl)-3-piperidyl 1511 N CH CH CH CH 1-(3-methylphenyl)-3-piperidyl 1512 N CH CH CH CH 1-(4-methylphenyl)-3-piperidyl 1513 N CH CH CH CH 1-(2-methoxyphenyl)-3-piperidyl 1514 N CH CH CH CH 1-(3-methoxyphenyl)-3-piperidyl 1515 N CH CH CH CH 1-(4-methoxyphenyl)-3-piperidyl 1516 N CH CH CH CH 1-(2-trifluoromethylphenyl)-3- piperidyl 1517 N CH CH CH CH 1-(3-trifluoromethylphenyl)-3- piperidyl 1518 N CH CH CH CH 1-(4-trifluoromethylphenyl)-3- piperidyl 1519 N CH CH CH CH 1-(3,5-difluorophenyl)-3- piperidyl 1520 N CH CH CH CH 1-(2-difluoromethoxyphenyl)-3- piperidyl 1521 N CH CH CH CH 1-(3-difluoromethoxyphenyl)-3- piperidyl 1522 N CH CH CH CH 1-(4-difluoromethoxyphenyl)-3- piperidyl 1523 N CH CH CH CH 1-(2-pyridyl)-3-piperidyl 1524 N CH CH CH CH 1-(3-pyridyl)-3-piperidyl 1525 N CH CH CH CH 1-(4-pyridyl)-3-piperidyl 1526 N CH CH CH CH 1-phenyl-4-piperidyl 1527 N CH CH CH CH 1-(2-fluorophenyl)-4-piperidyl 1528 N CH CH CH CH 1-(3-fluorophenyl)-4-piperidyl 1529 N CH CH CH CH 1-(4-fluorophenyl)-4-piperidyl 1530 N CH CH CH CH 1-(2-chlorophenyl)-4-piperidyl 1531 N CH CH CH CH 1-(3-chlorophenyl)-4-piperidyl 1532 N CH CH CH CH 1-(4-chlorophenyl)-4-piperidyl 1533 N CH CH CH CH 1-(2-methylphenyl)-4-piperidyl 1534 N CH CH CH CH 1-(3-methylphenyl)-4-piperidyl 1535 N CH CH CH CH 1-(4-methylphenyl)-4-piperidyl 1536 N CH CH CH CH 1-(2-methoxyphenyl)-4-piperidyl 1537 N CH CH CH CH 1-(3-methoxyphenyl)-4-piperidyl 1538 N CH CH CH CH 1-(4-methoxyphenyl)-4-piperidyl 1539 N CH CH CH CH 1-(2-trifluoromethylphenyl)-4- piperidyl 1540 N CH CH CH CH 1-(3-trifluoromethylphenyl)-4- piperidyl 1541 N CH CH CH CH 1-(4-trifluoromethylphenyl)-4- piperidyl 1542 N CH CH CH CH 1-(3,5-difluorophenyl)-4- piperidyl 1543 N CH CH CH CH 1-(2-difluoromethoxyphenyl)-4- piperidyl 1544 N CH CH CH CH 1-(3-difluoromethoxyphenyl)-4- piperidyl 1545 N CH CH CH CH 1-(4-difluoromethoxyphenyl)-4- piperidyl 1546 N CH CH CH CH 1-(2-pyridyl)-4-piperidyl 1547 N CH CH CH CH 1-(3-pyridyl)-4-piperidyl 1548 N CH CH CH CH 1-(4-pyridyl)-4-piperidyl 1549 N CH CH CH CH 3-hydroxymethyl-1-phenyl-4- piperidyl 1550 N CH CH CH CH 3-methoxycarbonyl-1-phenyl-4- piperidyl 1551 N CH CH CH CH 3-ethoxycarbonyl-1-phenyl-4- piperidyl 1552 N CH CH CH CH 3-isopropoxycarbonyl-1-phenyl-4- piperidyl 1553 N CH CH CH CH 4-phenylcyclohexyl 1554 N CH CH CH CH 4-(2-fluorophenyl)cyclohexyl 1555 N CH CH CH CH 4-(3-fluorophenyl)cyclohexyl 1556 N CH CH CH CH 4-(4-fluorophenyl)cyclohexyl 1557 N CH CH CH CH 4-(2-chlorophenyl)cyclohexyl 1558 N CH CH CH CH 4-(3-chlorophenyl)cyclohexyl 1559 N CH CH CH CH 4-(4-chlorophenyl)cyclohexyl 1560 N CH CH CH CH 4-(2-methylphenyl)cyclohexyl 1561 N CH CH CH CH 4-(3-methylphenyl)cyclohexyl 1562 N CH CH CH CH 4-(4-methylphenyl)cyclohexyl 1563 N CH CH CH CH 4-(2-methoxyphenyl)cyclohexyl 1564 N CH CH CH CH 4-(3-methoxyphenyl)cyclohexyl 1565 N CH CH CH CH 4-(4-methoxyphenyl)cyclohexyl 1566 N CH CH CH CH 4-(2-trifluoromethylphenyl)cyclo- hexyl 1567 N CH CH CH CH 4-(3-trifluoromethylphenyl)cyclo- hexyl 1568 N CH CH CH CH 4-(4-trifluoromethylphenyl)cyclo- hexyl 1569 N CH CH CH CH 4-(3,5-difluorophenyl)cyclohexyl 1570 N CH CH CH CH 4-(3-acetylphenyl)cyclohexyl 1571 N CH CH CH CH 4-(3-cyanophenyl)cyclohexyl 1572 N CH CH CH CH 4-(2-difluoromethoxyphenyl)cyclo- hexyl 1573 N CH CH CH CH 4-(3-difluoromethoxyphenyl)cyclo- hexyl 1574 N CH CH CH CH 4-(4-difluoromethoxyphenyl)cyclo- hexyl 1575 N CH CH CH CH 4-(2-pyridyl)cyclohexyl 1576 N CH CH CH CH 4-(3-pyridyl)cyclohexyl 1577 N CH CH CH CH 4-(4-pyridyl)cyclohexyl 1578 N CH CH CH CH 4-(4-fluoro-3-pyridyl)cyclohexyl 1579 N CH CH CH CH 4-(3-quinolyl)cyclohexyl 1580 N CH CH CH CH 4-(3-fluorophenyl)-4-hydroxy- cyclohexyl 1581 N CH CH CH CH 3-phenylcyclohexyl 1582 N CH CH CH CH 3-phenylcyclopentyl 1583 N CH CH CH CH 6-phenyl-3-tetrahydropyranyl 1584 N CH CH CH CH 6-(3-fluorophenyl)-3-tetrahydro- pyranyl 1585 N CH CH CH CH 2-phenylcyclopropyl 1586 N CH CH CH CH 2-(2-pyridyl)cyclopropyl 1587 N CH CH CH CH 2-(3-pyridyl)cyclopropyl 1588 N CH CH CH CH 2-(4-pyridyl)cyclopropyl 1589 N CH CH CH CH 2-(3-fluorophenyl)cyclopropyl 1590 N CH CH CH CH 2-indanyl 1591 N CH CH CH CH 2-tetrahydronaphthyl 1592 N CH CH CH CH 6-methoxy-2-tetrahydronaphthyl 1593 N CH CH CH CH benzyl 1594 N CH CH CH CH phenethyl 1595 N CH CH CH CH 3-phenylpropyl 1596 N CH CH CH CH 4-phenylbutyl 1597 N CH CH CH CH 2-methoxyphenethyl 1598 N CH CH CH CH 3-methoxyphenethyl 1599 N CH CH CH CH 4-methoxyphenethyl 1600 N CH CH CH CH 4-fluorophenethyl 1601 N CH CH CH CH 4-bromophenethyl 1602 N CH CH CH CH 4-chlorophenethyl 1603 N CH CH CH CH 3-trifluoromethylphenethyl 1604 N CH CH CH CH 3,4-dimethoxyphenethyl 1605 N CH CH CH CH 3-propoxyphenethyl 1606 N CH CH CH CH 3,5-difluorophenethyl 1607 N CH CH CH CH 4-dimethylaminophenethyl 1608 N CH CH CH CH 3-difluoromethoxyphenethyl 1609 N CH CH CH CH 2-methylphenethyl 1610 N CH CH CH CH 4-acetylphenethyl 1611 N CH CH CH CH 4-dimethylamino-2-methoxy- phenethyl 1612 N CH CH CH CH cyclohexylethyl 1613 N CH CH CH CH 2-(2-pyridyl)ethyl 1614 N CH CH CH CH 2-(3-pyridyl)ethyl 1615 N CH CH CH CH 2-(4-pyridyl)ethyl 1616 N CH CH CH CH 2-(2-quinolyl)ethyl 1617 N CH CH CH CH 2-(3-quinolyl)ethyl 1618 N CH CH CH CH 2-(4-quinolyl)ethyl 1619 N CH CH CH CH 2-(6-quinolyl)ethyl 1620 N CH CH CH CH 2-(2-indolyl)ethyl 1621 N CH CH CH CH 2-(3-indolyl)ethyl 1622 N CH CH CH CH 2-(7-aza-3-indolyl)ethyl 1623 N CH CH CH CH 2-(benzimidazolyl)ethyl 1624 N CH CH CH CH 2-(benzoxazolyl)ethyl 1625 N CH CH CH CH 2-(benzothiazolyl)ethyl 1626 N CH CH CH CH 2-(1-naphthyl)ethyl 1627 N CH CH CH CH 2-(2-naphthyl)ethyl 1628 N CH CH CH CH 1-(hydroxymethyl)-2-phenylethyl 1629 N CH CH CH CH 1-(methoxycarbonyl)-2-phenyl- ethyl 1630 N CH CH CH CH 1-(ethoxycarbonyl)-2-phenylethyl 1631 N CH CH CH CH 1-carboxy-2-phenylethyl 1632 N CH CH CH CH 1-(benzyloxycarbonyl)-2- phenylethyl 1633 N CH CH CH CH 1-(phenoxymethyl)-2-phenylethyl 1634 N CH CH CH CH 1-(benzyloxymethyl)-2-phenyl- ethyl 1635 N CH CH CH CH 1-(benzylcarbamoyl)-2-phenyl- ethyl 1636 N CH CH CH CH 1-(N-methylbenzylcarbamoyl)-2- phenylethyl 1637 N CH CH CH CH 1-(phenylcarbamoyl)-2-phenyl- ethyl 1638 N CH CH CH CH 1-(N-methylphenylcarbamoyl)-2- phenylethyl 1639 N CH CH CH CH 1-(N-benzylaminomethyl)-2- phenylethyl 1640 N CH CH CH CH 1-(N-benzyl-N-methylamino- methyl)-2-phenylethyl 1641 N CH CH CH CH 1-(anilinomethyl)-2-phenylethyl 1642 N CH CH CH CH 1-(N-methylanilinomethyl)-2- phenylethyl 1643 N CH CH CH CH 1-(N-methylaminomethyl)-2-phenyl- ethyl 1644 N CH CH CH CH 1-(N-ethylaminomethyl)-2-phenyl- ethyl 1645 N CH CH CH CH 1-(N-isobutylaminomethyl)-2- phenylethyl 1646 N CH CH CH CH 1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 1647 N CH CH CH CH 1-(aminomethyl)-2-phenylethyl 1648 N CH CH CH CH 1-benzyl-2-(2-pyridylmethyl- amino)ethyl 1649 N CH CH CH CH 1-benzyl-2-(3-pyridylmethyl- amino)ethyl 1650 N CH CH CH CH 1-benzyl-2-(4-pyridylmethyl- amino)ethyl 1651 N CH CH CH CH 2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 1652 N CH CH CH CH 2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 1653 N CH CH CH CH 2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 1654 N CH CH CH CH 2-hydroxy-2-phenylethyl 1655 N CH CH CH CH benzoylmethyl 1656 N CH CH CH CH 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 1657 N CH CH CH CH 1-(benzyloxycarbonyl)-2-cyclo- hexylethyl 1658 N CH CH CH CH 1-(phenoxymethyl)-2-(3- indolyl)ethyl 1659 N CH CH CH CH 2-(2-methoxyphenoxy)ethyl 1660 N CH CH CH CH 1-(benzylcarbamoyl)-2-cyclo- hexylethyl 1661 N CH CH CH CH 1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 1662 N CH CH CH CH 1-(phenylcarbamoyl)-2-cyclohexyl- ethyl 1663 N CH CH CH CH 1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 1664 N CH CH CH CH 1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 1665 N CH CH CH CH 1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 1666 N CH CH CH CH 1-(benzylcarbamoyl)-2-(4- pyridyl)ethyl 1667 N CH CH CH CH 1-(4-pyridylmethylcarbamoyl)-2-(4- fluorophenyl)ethyl 1668 N CH CH CH CH 1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 1669 N CH CH CH CH 1-(benzyloxymethyl)-2-(2- indolyl)ethyl 1670 N CH CH CH CH 1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 1671 N CH CH CH CH 1-(N-methylbenzylcarbamoyl)-2- (3-pyridyl)ethyl 1672 N CH CH CH CH 2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 1673 N CH CH CH CH 2-hydroxy-2-(2-quinolyl)ethyl 1674 N CH CH CH CH 2-hydroxy-2-(3-quinolyl)ethyl 1675 N CH CH CH CH 2-hydroxy-2-(4-quinolyl)ethyl 1676 N CH CH CH CH 2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 1677 N CH CH CH CH 1-carboxy-2-cyclohexylethyl 1678 N CH CH CH CH 2-hydroxy-2-(6-quinolyl)ethyl 1679 N CH CH CH CH 2-(benzylamino)-2-phenylethyl 1680 N CH CH CH CH 2-amino-2-(2-naphthyl)propyl 1681 N CH CH CH CH 2-(phenylamino)ethyl 1682 N CH CH CH CH diphenylmethyl 1683 N CH CH CH CH 2,2-diphenylethyl 1684 N CH CH CH CH 2-phenyl-2-(2-pyridyl)ethyl 1685 N CH CH CH CH 2-phenyl-2-(3-pyridyl)ethyl 1686 N CH CH CH CH 2-phenyl-2-(4-pyridyl)ethyl 1687 N CH CH CH CH 2-phenoxy-2-phenylethyl 1688 N CH CH CH CH 2-(benzyloxy)-2-phenylethyl 1689 N CH CH CH N 1-phenyl-3-pyrrolidinyl 1690 N CH CH CH N 1-(2-fluorophenyl)-3-pyrrolidinyl 1691 N CH CH CH N 1-(3-fluorophenyl)-3-pyrrolidinyl 1692 N CH CH CH N 1-(4-fluorophenyl)-3-pyrrolidinyl 1693 N CH CH CH N 1-(2-chlorophenyl)-3-pyrrolidinyl 1694 N CH CH CH N 1-(3-chlorophenyl)-3-pyrrolidinyl 1695 N CH CH CH N 1-(4-chlorophenyl)-3-pyrrolidinyl 1696 N CH CH CH N 1-(2-methylphenyl)-3-pyrrolidinyl 1697 N CH CH CH N 1-(3-methylphenyl)-3-pyrrolidinyl 1698 N CH CH CH N 1-(4-methylphenyl)-3-pyrrolidinyl 1699 N CH CH CH N 1-(2-methoxyphenyl)-3- pyrrolidinyl 1700 N CH CH CH N 1-(3-methoxyphenyl)-3- pyrrolidinyl 1701 N CH CH CH N 1-(4-methoxyphenyl)-3- pyrrolidinyl 1702 N CH CH CH N 1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 1703 N CH CH CH N 1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 1704 N CH CH CH N 1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 1705 N CH CH CH N 1-(3,5-difluorophenyl)-3- pyrrolidinyl 1706 N CH CH CH N 1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 1707 N CH CH CH N 1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 1708 N CH CH CH N 1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 1709 N CH CH CH N 1-(2-pyridyl)-3-pyrrolidinyl 1710 N CH CH CH N 1-(3-pyridyl)-3-pyrrolidinyl 1711 N CH CH CH N 1-(4-pyridyl)-3-pyrrolidinyl 1712 N CH CH CH N 1-(2-pyrimidinyl)-3-pyrrolidinl 1713 N CH CH CH N 5-oxo-1-phenyl-3-pyrrolidinyl 1714 N CH CH CH N 1-phenyl-3-piperidyl 1715 N CH CH CH N 1-(2-fluorophenyl)-3-piperidyl 1716 N CH CH CH N 1-(3-fluorophenyl)-3-piperidyl 1717 N CH CH CH N 1-(4-fluorophenyl)-3-piperidyl 1718 N CH CH CH N 1-(2-chlorophenyl)-3-piperidyl 1719 N CH CH CH N 1-(3-chlorophenyl)-3-piperidyl 1720 N CH CH CH N 1-(4-chlorophenyl)-3-piperidyl 1721 N CH CH CH N 1-(2-methylphenyl)-3-piperidyl 1722 N CH CH CH N 1-(3-methylphenyl)-3-piperidyl 1723 N CH CH CH N 1-(4-methylphenyl)-3-piperidyl 1724 N CH CH CH N 1-(2-methoxyphenyl)-3-piperidyl 1725 N CH CH CH N 1-(3-methoxyphenyl)-3-piperidyl 1726 N CH CH CH N 1-(4-methoxyphenyl)-3-piperidyl 1727 N CH CH CH N 1-(2-trifuoromethylphenyl)-3- piperidyl 1728 N CH CH CH N 1-(3-trifuoromethylphenyl)-3- piperidyl 1729 N CH CH CH N 1-(4-trifuoromethylphenyl)-3- piperidyl 1730 N CH CH CH N 1-(3,5-difluorophenyl)-3-piperidyl 1731 N CH CH CH N 1-(2-difluoromethoxyphenyl)-3- piperidyl 1732 N CH CH CH N 1-(3-difluoromethoxyphenyl)-3- piperidyl 1733 N CH CH CH N 1-(4-difluoromethoxyphenyl)-3- piperidiyl 1734 N CH CH CH N 1-(2-pyridyl)-3-piperidyl 1735 N CH CH CH N 1-(3-pyridyl)-3-piperidyl 1736 N CH CH CH N 1-(4-pyridyl)-3-piperidyl 1737 N CH CH CH N 1-phenyl-4-piperidyl 1738 N CH CH CH N 1-(2-fluorophenyl)-4-piperidyl 1739 N CH CH CH N 1-(3-fluorophenyl)-4-piperidyl 1740 N CH CH CH N 1-(4-fluorophenyl)-4-piperidyl 1741 N CH CH CH N 1-(2-chlorophenyl)-4-piperidyl 1742 N CH CH CH N 1-(3-chlorophenyl)-4-piperidyl 1743 N CH CH CH N 1-(4-chlorophenyl)-4-piperidyl 1744 N CH CH CH N 1-(2-methylphenyl)-4-piperidyl 1745 N CH CH CH N 1-(3-methylphenyl)-4-piperidyl 1746 N CH CH CH N 1-(4-methylphenyl)-4-piperidyl 1747 N CH CH CH N 1-(2-methoxyphenyl)-4-piperidyl 1748 N CH CH CH N 1-(3-methoxyphenyl)-4-piperidyl 1749 N CH CH CH N 1-(4-methoxyphenyl)-4-piperidyl 1750 N CH CH CH N 1-(2-trifluoromethylphenyl)-4- piperidyl 1751 N CH CH CH N 1-(3-trifluoromethylphenyl)-4- piperidyl 1752 N CH CH CH N 1-(4-trifluoromethylphenyl)-4- piperidyl 1753 N CH CH CH N 1-(3,5-difluorophenyl)-4- piperidyl 1754 N CH CH CH N 1-(2-difluoromethoxyphenyl)-4- piperidyl 1755 N CH CH CH N 1-(3-difluoromethoxyphenyl)-4- piperidyl 1756 N CH CH CH N 1-(4-difluoromethoxyphenyl)-4- piperidyl 1757 N CH CH CH N 1-(2-pyridyl)-4-piperidyl 1758 N CH CH CH N 1-(3-pyridyl)-4-piperidyl 1759 N CH CH CH N 1-(4-pyridyl)-4-piperidyl 1760 N CH CH CH N 3-hydroxymethyl-1-phenyl-4- piperidyl 1761 N CH CH CH N 3-methoxycarbonyl-1-phenyl-4- piperidyl 1762 N CH CH CH N 3-ethoxycarbonyl-1-phenyl-4- piperidyl 1763 N CH CH CH N 3-isopropoxycarbonyl-1-phenyl-4- piperidyl 1764 N CH CH CH N 4-phenylcyclohexyl 1765 N CH CH CH N 4-(2-fluorophenyl)cyclohexyl 1766 N CH CH CH N 4-(3-fluorophenyl)cyclohexyl 1767 N CH CH CH N 4-(4-fluorophenyl)cyclohexyl 1768 N CH CH CH N 4-(2-chlorophenyl)cyclohexyl 1769 N CH CH CH N 4-(3-chlorophenyl)cyclohexyl 1770 N CH CH CH N 4-(4-chlorophenyl)cyclohexyl 1771 N CH CH CH N 4-(2-methylphenyl)cyclohexyl 1772 N CH CH CH N 4-(3-methylphenyl)cyclohexyl 1773 N CH CH CH N 4-(4-methylphenyl)cyclohexyl 1774 N CH CH CH N 4-(2-methoxyphenyl)cyclohexyl 1775 N CH CH CH N 4-(3-methoxyphenyl)cyclohexyl 1776 N CH CH CH N 4-(4-methoxyphenyl)cyclohexyl 1777 N CH CH CH N 4-(2-trifluoromethylphenyl)cyclo- hexyl 1778 N CH CH CH N 4-(3-trifluoromethylphenyl)cyclo- hexyl 1779 N CH CH CH N 4-(4-trifluoromethylphenyl)cyclo- hexyl 1780 N CH CH CH N 4-(3,5-difluorophenyl)cyclohexyl 1781 N CH CH CH N 4-(3-acetylphenyl)cyclohexyl 1782 N CH CH CH N 4-(3-cyanophenyl)cyclohexyl 1783 N CH CH CH N 4-(2-difluoromethoxyphenyl)cyclo- hexyl 1784 N CH CH CH N 4-(3-difluoromethoxyphenyl)cyclo- hexyl 1785 N CH CH CH N 4-(4-difluoromethoxyphenyl)cyclo- hexyl 1786 N CH CH CH N 4-(2-pyridyl)cyclohexyl 1787 N CH CH CH N 4-(3-pyridyl)cyclohexyl 1788 N CH CH CH N 4-(4-pyridyl)cyclohexyl 1789 N CH CH CH N 4-(4-fluoro-3-pyridyl)cyclohexyl 1790 N CH CH CH N 4-(3-quinolyl)cyclohexyl 1791 N CH CH CH N 4-(3-fluorophenyl)-4-hydroxy- cyclohexyl 1792 N CH CH CH N 3-phenylcyclohexyl 1793 N CH CH CH N 3-phenylcyclopentyl 1794 N CH CH CH N 6-phenyl-3-tetrahydropyranyl 1795 N CH CH CH N 6-(3-fluorophenyl)-3-tetrahydro- pyranyl 1796 N CH CH CH N 2-phenylcyclopropyl 1797 N CH CH CH N 2-(2-pyridyl)cyclopropyl 1798 N CH CH CH N 2-(3-pyridyl)cyclopropyl 1799 N CH CH CH N 2-(4-pyridyl)cyclopropyl 1800 N CH CH CH N 2-(3-fluorophenyl)cyclopropyl 1801 N CH CH CH N 2-indanyl 1802 N CH CH CH N 2-tetrahydronaphthyl 1803 N CH CH CH N 6-methoxy-2-tetrahydronaphthyl 1804 N CH CH CH N benzyl 1805 N CH CH CH N phenethyl 1806 N CH CH CH N 3-phenylpropyl 1807 N CH CH CH N 4-phenylbutyl 1808 N CH CH CH N 2-methoxyphenethyl 1809 N CH CH CH N 3-methoxyphenethyl 1810 N CH CH CH N 4-methoxyphenethyl 1811 N CH CH CH N 4-f luorophenethyl 1812 N CH CH CH N 4-bromophenethyl 1813 N CH CH CH N 4-chlorophenethyl 1814 N CH CH CH N 3-trifluoromethylphenethyl 1815 N CH CH CH N 3,4-dimethoxyphenethyl 1816 N CH CH CH N 3-propoxyphenethyl 1817 N CH CH CH N 3,5-difluorophenethyl 1818 N CH CH CH N 4-dimethylaminophenethyl 1819 N CH CH CH N 3-difluoromethoxyphenethyl 1820 N CH CH CH N 2-methylphenethyl 1821 N CH CH CH N 4-acetylphenethyl 1822 N CH CH CH N 4-dimethylamino-2-methoxy- phenethyl 1823 N CH CH CH N cyclohexylethyl 1824 N CH CH CH N 2-(2-pyridyl)ethyl 1825 N CH CH CH N 2-(3-pyridyl)ethyl 1826 N CH CH CH N 2-(4-pyridyl)ethyl 1827 N CH CH CH N 2-(2-quinolyl)ethyl 1828 N CH CH CH N 2-(3-quinolyl)ethyl 1829 N CH CH CH N 2-(4-quinolyl)ethyl 1830 N CH CH CH N 2-(6-quinolyl)ethyl 1831 N CH CH CH N 2-(2-indolyl)ethyl 1832 N CH CH CH N 2-(3-indolyl)ethyl 1833 N CH CH CH N 2-(7-aza-3-indolyl)ethyl 1834 N CH CH CH N 2-(benzimidazolyl)ethyl 1835 N CH CH CH N 2-(benzoxazolyl)ethyl 1836 N CH CH CH N 2-(benzothiazolyl)ethyl 1837 N CH CH CH N 2-(1-naphthyl)ethyl 1838 N CH CH CH N 2-(2-naphthyl)ethyl 1839 N CH CH CH N 1-(hydroxymethyl)-2-phenylethyl 1840 N CH CH CH N 1-(methoxycarbonyl)-2-phenylethyl 1841 N CH CH CH N 1-(ethoxycarbonyl)-2-phenylethyl 1842 N CH CH CH N 1-carboxy-2-phenylethyl 1843 N CH CH CH N 1-(benzyloxycarbonyl)-2-phenyl- ethyl 1844 N CH CH CH N 1-(phenoxymethyl)-2-phenylethyl 1845 N CH CH CH N 1-(benzyloxymethyl)-2-phenylethyl 1846 N CH CH CH N 1-(benzylcarbamoyl)-2-phenylethyl 1847 N CH CH CH N 1-(N-methylbenzylcarbamoyl)-2- phenylethyl 1848 N CH CH CH N 1-(phenylcarbamoyl)-2-phenylethyl 1849 N CH CH CH N 1-(N-methylphenylcarbamoyl)-2- phenylethyl 1850 N CH CH CH N 1-(N-benzylaminomethyl)-2- phenylethyl 1851 N CH CH CH N 1-(N-benzyl-N-methylaminomethyl)- 2-phenylethyl 1852 N CH CH CH N 1-(anilinomethyl)-2-phenylethyl 1853 N CH CH CH N 1-(N-methylanilinomethyl)-2- phenylethyl 1854 N CH CH CH N 1-(N-methylaminomethyl)-2- phenylethyl 1855 N CH CH CH N 1-(N-ethylaminomethyl)-2- phenylethyl 1856 N CH CH CH N 1-(N-isobutylaminomethyl)-2- phenylethyl 1857 N CH CH CH N 1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 1858 N CH CH CH N 1-(aminomethyl)-2-phenylethyl 1859 N CH CH CH N 1-benzyl-2-(2-pyridylmethyl- amino)ethyl 1860 N CH CH CH N 1-benzyl-2-(3-pyridylmethyl- amino)ethyl 1861 N CH CH CH N 1-benzyl-2-(4-pyridylmethyl- amino)ethyl 1862 N CH CH CH N 2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 1863 N CH CH CH N 2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 1864 N CH CH CH N 2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 1865 N CH CH CH N 2-hydroxy-2-phenylethyl 1866 N CH CH CH N benzoylmethyl 1867 N CH CH CH N 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 1868 N CH CH CH N 1-(benzyloxycarbonyl)-2- cyclohexylethyl 1869 N CH CH CH N 1-(phenoxymethyl)-2-(3- indolyl)ethyl 1870 N CH CH CH N 2-(2-methoxyphenoxy)ethyl 1871 N CH CH CH N 1-(benzylcarbamoyl)-2- cyclohexylethyl 1872 N CH CH CH N 1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 1873 N CH CH CH N 1-(phenylcarbamoyl)-2- cyclohexylethyl 1874 N CH CH CH N 1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 1875 N CH CH CH N 1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 1876 N CH CH CH N 1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 1877 N CH CH CH N 1-(benzylcarbamoyl)-2-(4- pyridyl)ethyl 1878 N CH CH CH N 1-(4-pyridylmethylcarbamoyl)-2-(4- fluorophenyl)ethyl 1879 N CH CH CH N 1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 1880 N CH CH CH N 1-(benzyloxymethyl)-2-(2- indolyl)ethyl 1881 N CH CH CH N 1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 1882 N CH CH CH N 1-(N-methylbenzylcarbamoyl)-2-(3- pyridyl)ethyl 1883 N CH CH CH N 2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 1884 N CH CH CH N 2-hydroxy-2-(2-quinolyl)ethyl 1885 N CH CH CH N 2-hydroxy-2-(3-quinolyl)ethyl 1886 N CH CH CH N 2-hydroxy-2-(4-quinolyl)ethyl 1887 N CH CH CH N 2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 1888 N CH CH CH N 1-carboxy-2-cyclohexylethyl 1889 N CH CH CH N 2-hydroxy-2-(6-quinolyl)ethyl 1890 N CH CH CH N 2-(benzylamino)-2-phenylethyl 1891 N CH CH CH N 2-amino-2-(2-naphthyl)propyl 1892 N CH CH CH N 2-(phenylamino)ethyl 1893 N CH CH CH N diphenylmethyl 1894 N CH CH CH N 2,2-diphenylethyl 1895 N CH CH CH N 2-phenyl-2-(2-pyridyl)ethyl 1896 N CH CH CH N 2-phenyl-2-(3-pyridyl)ethyl 1897 N CH CH CH N 2-phenyl-2-(4-pyridyl)ethyl 1898 N CH CH CH N 2-phenoxy-2-phenylethyl 1899 N CH CH CH N 2-(benzyloxy)-2-phenylethyl 1900 CH N CH CH CH 1-phenyl-3-pyrrolidinyl 1901 CH N CH CH CH 1-(2-fluorophenyl)-3-pyrrolidinyl 1902 CH N CH CH CH 1-(3-fluorophenyl)-3-pyrrolidinyl 1903 CH N CH CH CH 1-(4-fluorophenyl)-3-pyrrolidinyl 1904 CH N CH CH CH 1-(2-chlorophenyl)-3-pyrrolidinyl 1905 CH N CH CH CH 1-(3-chlorophenyl)-3-pyrrolidinyl 1906 CH N CH CH CH 1-(4-chlorophenyl)-3-pyrrolidinyl 1907 CH N CH CH CH 1-(2-methylphenyl)-3-pyrrolidinyl 1908 CH N CH CH CH 1-(3-methylphenyl)-3-pyrrolidinyl 1909 CH N CH CH CH 1-(4-methylphenyl)-3-pyrrolidinyl 1910 CH N CH CH CH 1-(2-methoxyphenyl)-3-pyrrolidinyl 1911 CH N CH CH CH 1-(3-methoxyphenyl)-3-pyrrolidinyl 1912 CH N CH CH CH 1-(4-methoxyphenyl)-3-pyrrolidinyl 1913 CH N CH CH CH 1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 1914 CH N CH CH CH 1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 1915 CH N CH CH CH 1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 1916 CH N CH CH CH 1-(3,5-difluorophenyl)-3- pyrrolidinyl 1917 CH N CH CH CH 1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 1918 CH N CH CH CH 1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 1919 CH N CH CH CH 1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 1920 CH N CH CH CH 1-(2-pyridyl)-3-pyrrolidinyl 1921 CH N CH CH CH 1-(3-pyridyl)-3-pyrrolidinyl 1922 CH N CH CH CH 1-(4-pyridyl)-3-pyrrolidinyl 1923 CH N CH CH CH 1-(2-pyrimidinyl)-3-pyrrolidinyl 1924 CH N CH CH CH 5-oxo-1-phenyl-3-pyrrolidinyl 1925 CH N CH CH CH 1-phenyl-3-piperidyl 1926 CH N CH CH CH 1-(2-fluorophenyl)-3-piperidyl 1927 CH N CH CH CH 1-(3-fluorophenyl)-3-piperidyl 1928 CH N CH CH CH 1-(4-fluorophenyl)-3-piperidyl 1929 CH N CH CH CH 1-(2-chlorophenyl)-3-piperidyl 1930 CH N CH CH CH 1-(3-chlorophenyl)-3-piperidyl 1931 CH N CH CH CH 1-(4-chlorophenyl)-3-piperidyl 1932 CH N CH CH CH 1-(2-methylphenyl)-3-piperidyl 1933 CH N CH CH CH 1-(3-methylphenyl)-3-piperidyl 1934 CH N CH CH CH 1-(4-methylphenyl)-3-piperidyl 1935 CH N CH CH CH 1-(2-methoxyphenyl)-3-piperidyl 1936 CH N CH CH CH 1-(3-methoxyphenyl)-3-piperidyl 1937 CH N CH CH CH 1-(4-methoxyphenyl)-3-piperidyl 1938 CH N CH CH CH 1-(2-trifluoromethylphenyl)-3- piperidyl 1939 CH N CH CH CH 1-(3-trifluoromethylphenyl)-3- piperidyl 1940 CH N CH CH CH 1-(4-trifluoromethylphenyl)-3- piperidyl 1941 CH N CH CH CH 1-(3,5-difluorophenyl)-3- piperidyl 1942 CH N CH CH CH 1-(2-difluoromethoxyphenyl)-3- piperidyl 1943 CH N CH CH CH 1-(3-difluoromethoxyphenyl)-3- piperidyl 1944 CH N CH CH CH 1-(4-difluoromethoxyphenyl)-3- piperidyl 1945 CH N CH CH CH 1-(2-pyridyl)-3-piperidyl 1946 CH N CH CH CH 1-(3-pyridyl)-3-piperidyl 1947 CH N CH CH CH 1-(4-pyridyl)-3-piperidyl 1948 CH N CH CH CH 1-phenyl-4-piperidyl 1949 CH N CH CH CH 1-(2-fluorophenyl)-4-piperidyl 1950 CH N CH CH CH 1-(3-fluorophenyl)-4-piperidyl 1951 CH N CH CH CH 1-(4-fluorophenyl)-4-piperidyl 1952 CH N CH CH CH 1-(2-chlorophenyl)-4-piperidyl 1953 CH N CH CH CH 1-(3-chlorophenyl)-4-piperidyl 1954 CH N CH CH CH 1-(4-chlorophenyl)-4-piperidyl 1955 CH N CH CH CH 1-(2-methylphenyl)-4-piperidyl 1956 CH N CH CH CH 1-(3-methylphenyl)-4-piperidyl 1957 CH N CH CH CH 1-(4-methylphenyl)-4-piperidyl 1958 CH N CH CH CH 1-(2-methoxyphenyl)-4-piperidyl 1959 CH N CH CH CH 1-(3-methoxyphenyl)-4-piperidyl 1960 CH N CH CH CH 1-(4-methoxyphenyl)-4-piperidyl 1961 CH N CH CH CH 1-(2-trifluoromethylphenyl)-4- piperidyl 1962 CH N CH CH CH 1-(3-trifluoromethylphenyl)-4- piperidyl 1963 CH N CH CH CH 1-(4-trifluoromethylphenyl)-4- piperidyl 1964 CH N CH CH CH 1-(3,5-difluorophenyl)-4-piperidyl 1965 CH N CH CH CH 1-(2-difluoromethoxyphenyl)-4- piperidyl 1966 CH N CH CH CH 1-(3-difluoromethoxyphenyl)-4- piperidyl 1967 CH N CH CH CH 1-(4-difluoromethoxyphenyl)-4- piperidyl 1968 CH N CH CH CH 1-(2-pyridyl)-4-piperidyl 1969 CH N CH CH CH 1-(3-pyridyl)-4-piperidyl 1970 CH N CH CH CH 1-(4-pyridyl)-4-piperidyl 1971 CH N CH CH CH 3-hydroxymethyl-1-phenyl-4- piperidyl 1972 CH N CH CH CH 3-methoxycarbonyl-1-phenyl-4- piperidyl 1973 CH N CH CH CH 3-ethoxycarbonyl-1-phenyl-4- piperidyl 1974 CH N CH CH CH 3-isopropoxycarbonyl-1-phenyl-4- piperidyl 1975 CH N CH CH CH 4-phenylcyclohexyl 1976 CH N CH CH CH 4-(2-fluorophenyl)cyclohexyl 1977 CH N CH CH CH 4-(3-fluorophenyl)cyclohexyl 1978 CH N CH CH CH 4-(4-fluorophenyl)cyclohexyl 1979 CH N CH CH CH 4-(2-chlorophenyl)cyclohexyl 1980 CH N CH CH CH 4-(3-chlorophenyl)cyclohexyl 1981 CH N CH CH CH 4-(4-chlorophenyl)cyclohexyl 1982 CH N CH CH CH 4-(2-methylphenyl)cyclohexyl 1983 CH N CH CH CH 4-(3-methylphenyl)cyclohexyl 1984 CH N CH CH CH 4-(4-methylphenyl)cyclohexyl 1985 CH N CH CH CH 4-(2-methoxyphenyl)cyclohexyl 1986 CH N CH CH CH 4-(3-methoxyphenyl)cyclohexyl 1987 CH N CH CH CH 4-(4-methoxyphenyl)cyclohexyl 1988 CH N CH CH CH 4-(2-trifluoromethylphenyl)cyclo- hexyl 1989 CH N CH CH CH 4-(3-trifluoromethylphenyl)cyclo- hexyl 1990 CH N CH CH CH 4-(4-trifluoromethylphenyl)cyclo- hexyl 1991 CH N CH CH CH 4-(3,5-difluorophenyl)cyclohexyl 1992 CH N CH CH CH 4-(3-acetylphenyl)cyclohexyl 1993 CH N CH CH CH 4-(3-cyanophenyl)cyclohexyl 1994 CH N CH CH CH 4-(2-difluoromethoxyphenyl)cyclo- hexyl 1995 CH N CH CH CH 4-(3-difluoromethoxyphenyl)cyclo- hexyl 1996 CH N CH CH CH 4-(4-difluoromethoxyphenyl)cyclo- hexyl 1997 CH N CH CH CH 4-(2-pyridyl)cyclohexyl 1998 CH N CH CH CH 4-(3-pyridyl)cyclohexyl 1999 CH N CH CH CH 4-(4-pyridyl)cyclohexyl 2000 CH N CH CH CH 4-(4-fluoro-3-pyridyl)cyclohexyl 2001 CH N CH CH CH 4-(3-quinolyl)cyclohexyl 2002 CH N CH CH CH 4-(3-fluorophenyl)-4-hydroxy- cyclohexyl 2003 CH N CH CH CH 3-phenylcyclohexyl 2004 CH N CH CH CH 3-phenylcyclopentyl 2005 CH N CH CH CH 6-phenyl-3-tetrahydropyranyl 2006 CH N CH CH CH 6-(3-fluorophenyl)-3-tetrahydro- pyranyl 2007 CH N CH CH CH 2-phenylcyclopropyl 2008 CH N CH CH CH 2-(2-pyridyl)cyclopropyl 2009 CH N CH CH CH 2-(3-pyridyl)cyclopropyl 2010 CH N CH CH CH 2-(4-pyridyl)cyclopropyl 2011 CH N CH CH CH 2-(3-fluorophenyl)cyclopropyl 2012 CH N CH CH CH 2-indanyl 2013 CH N CH CH CH 2-tetrahydronaphthyl 2014 CH N CH CH CH 6-methoxy-2-tetrahydronaphthyl 2015 CH N CH CH CH benzyl 2016 CH N CH CH CH phenethyl 2017 CH N CH CH CH 3-phenylpropyl 2018 CH N CH CH CH 4-phenylbutyl 2019 CH N CH CH CH 2-methoxyphenethyl 2020 CH N CH CH CH 3-methoxyphenethyl 2021 CH N CH CH CH 4-methoxyphenethyl 2022 CH N CH CH CH 4-fluorophenethyl 2023 CH N CH CH CH 4-bromophenethyl 2024 CH N CH CH CH 4-chlorophenethyl 2025 CH N CH CH CH 3-trifluoromethylphenethyl 2026 CH N CH CH CH 3,4-dimethoxyphenethyl 2027 CH N CH CH CH 3-propoxyphenethyl 2028 CH N CH CH CH 3,5-difluorophenethyl 2029 CH N CH CH CH 4-dimethylaminophenethyl 2030 CH N CH CH CH 3-difluoromethoxyphenethyl 2031 CH N CH CH CH 2-methylphenethyl 2032 CH N CH CH CH 4-acetylphenethyl 2033 CH N CH CH CH 4-dimethylamino-2-methoxyphenethyl 2034 CH N CH CH CH cyclohexylethyl 2035 CH N CH CH CH 2-(2-pyridyl)ethyl 2036 CH N CH CH CH 2-(3-pyridyl)ethyl 2037 CH N CH CH CH 2-(4-pyridyl)ethyl 2038 CH N CH CH CH 2-(2-quinolyl)ethyl 2039 CH N CH CH CH 2-(3-quinolyl)ethyl 2040 CH N CH CH CH 2-(4-quinolyl)ethyl 2041 CH N CH CH CH 2-(6-quinolyl)ethyl 2042 CH N CH CH CH 2-(2-indolyl)ethyl 2043 CH N CH CH CH 2-(3-indolyl)ethyl 2044 CH N CH CH CH 2-(7-aza-3-indolyl)ethyl 2045 CH N CH CH CH 2-(benzimidazolyl)ethyl 2046 CH N CH CH CH 2-(benzoxazolyl)ethyl 2047 CH N CH CH CH 2-(benzothiazolyl)ethyl 2048 CH N CH CH CH 2-(1-naphthyl)ethyl 2049 CH N CH CH CH 2-(2-naphthyl)ethyl 2050 CH N CH CH CH 1-(hydroxymethyl)-2-phenylethyl 2051 CH N CH CH CH 1-(methoxycarbonyl)-2-phenylethyl 2052 CH N CH CH CH 1-(ethoxycarbonyl)-2-phenylethyl 2053 CH N CH CH CH 1-carboxy-2-phenylethyl 2054 CH N CH CH CH 1-(benzyloxycarbonyl)-2- phenylethyl 2055 CH N CH CH CH 1-(phenoxymethyl)-2-phenylethyl 2056 CH N CH CH CH 1-(benzyloxymethyl)-2-phenylethyl 2057 CH N CH CH CH 1-(benzylcarbamoyl)-2-phenylethyl 2058 CH N CH CH CH 1-(N-methylbenzylcarbamoyl)-2- phenylethyl 2059 CH N CH CH CH 1-(phenylcarbantoyl)-2-phenylethyl 2060 CH N CH CH CH 1-(N-methylphenylcarbamoyl)-2- phenylethyl 2061 CH N CH CH CH 1-(N-benzylaminomethyl)-2- phenylethyl 2062 CH N CH CH CH 1-(N-benzyl-N-methylaminomethyl)- 2-phenylethyl 2063 CH N CH CH CH 1-(anilinomethyl)-2-phenylethyl 2064 CH N CH CH CH 1-(N-methylanilinomethyl)-2- phenylethyl 2065 CH N CH CH CH 1-(N-methylaminomethyl)-2- phenylethyl 2066 CH N CH CH CH 1-(N-ethylaminomethyl)-2- phenylethyl 2067 CH N CH CH CH 1-(N-isobutylaminomethyl)-2- phenylethyl 2068 CH N CH CH CH 1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 2069 CH N CH CH CH 1-(aminomethyl)-2-phenylethyl 2070 CH N CH CH CH 1-benzyl-2-(2-pyridylmethyl- 2-amino)ethyl 2071 CH N CH CH CH 1-benzyl-2-(3-pyridylmethyl- 2-amino)ethyl 2072 CH N CH CH CH 1-benzyl-2-(4-pyridylmethyl- 2-amino)ethyl 2073 CH N CH CH CH 2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 2074 CH N CH CH CH 2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 2075 CH N CH CH CH 2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 2076 CH N CH CH CH 2-hydroxy-2-phenylethyl 2077 CH N CH CH CH benzoylmethyl 2078 CH N CH CH CH 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 2079 CH N CH CH CH 1-(benzyloxycarbonyl)-2- cyclohexylethyl 2080 CH N CH CH CH 1-(phenoxymethyl)-2-(3- indolyl)ethyl 2081 CH N CH CH CH 2-(2-methoxyphenoxy)ethyl 2082 CH N CH CH CH 1-(benzylcarbamoyl)-2-cyclohexyl- ethyl 2083 CH N CH CH CH 1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 2084 CH N CH CH CH 1-(phenylcarbamoyl)-2-cyclohexyl- ethyl 2085 CH N CH CH CH 1-(N-methylphenylcarbaxnoyl)-2- cyclohexylethyl 2086 CH N CH CH CH 1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 2087 CH N CH CH CH 1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 2088 CH N CH CH CH 1-(benzylcarbanioyl)-2-(4- pyridyl)ethyl 2089 CH N CH CH CH 1-(4-pyridylmethylcarbamoyl)-2-(4- fluorophenyl)ethyl 2090 CH N CH CH CH 1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 2091 CH N CH CH CH 1-(benzyloxymethyl)-2-(2- indolyl)ethyl 2092 CH N CH CH CH 1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 2093 CH N CH CH CH 1-(N-methylbenzylcarbamoyl)-2-(3- pyridyl)ethyl 2094 CH N CH CH CH 2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 2095 CH N CH CH CH 2-hydroxy-2-(2-quinolyl)ethyl 2096 CH N CH CH CH 2-hydroxy-2-(3-quinolyl)ethyl 2097 CH N CH CH CH 2-hydroxy-2-(4-quinolyl)ethyl 2098 CH N CH CH CH 2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 2099 CH N CH CH CH 1-carboxy-2-cyclohexylethyl 2100 CH N CH CH CH 2-hydroxy-2-(6-quinolyl)ethyl 2101 CH N CH CH CH 2-(benzylamino)-2-phenylethyl 2102 CH N CH CH CH 2-amino-2-(2-naphthyl)propyl 2103 CH N CH CH CH 2-(phenylamino)ethyl 2104 CH N CH CH CH diphenylmethyl 2105 CH N CH CH CH 2,2-diphenylethyl 2106 CH N CH CH CH 2-phenyl-2-(2-pyridyl)ethyl 2107 CH N CH CH CH 2-phenyl-2-(3-pyridyl)ethyl 2108 CH N CH CH CH 2-phenyl-2-(4-pyridyl)ethyl 2109 CH N CH CH CH 2-phenoxy-2-phenylethyl 2110 CH N CH CH CH 2-(benzyloxy)-2-phenylethyl 2111 CH N CH CH N 1-phenyl-3-pyrrolidinyl 2112 CH N CH CH N 1-(2-fluorophenyl)-3-pyrrolidinyl 2113 CH N CH CH N 1-(3-fluorophenyl)-3-pyrrolidinyl 2114 CH N CH CH N 1-(4-fluorophenyl)-3-pyrrolidinyl 2115 CH N CH CH N 1-(2-chlorophenyl)-3-pyrrolidinyl 2116 CH N CH CH N 1-(3-chlorophenyl)-3-pyrrolidinyl 2117 CH N CH CH N 1-(4-chlorophenyl)-3-pyrrolidinyl 2118 CH N CH CH N 1-(2-methylphenyl)-3-pyrrolidinyl 2119 CH N CH CH N 1-(3-methylphenyl)-3-pyrrolidinyl 2120 CH N CH CH N 1-(4-methylphenyl)-3-pyrrolidinyl 2121 CH N CH CH N 1-(2-methoxyphenyl)-3-pyrrolidinyl 2122 CH N CH CH N 1-(3-methoxyphenyl)-3-pyrrolidinyl 2123 CH N CH CH N 1-(4-methoxyphenyl)-3-pyrrolidinyl 2124 CH N CH CH N 1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 2125 CH N CH CH N 1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 2126 CH N CH CH N 1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 2127 CH N CH CH N 1-(3,5-difluorophenyl)-3- pyrrolidinyl 2128 CH N CH CH N 1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 2129 CH N CH CH N 1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 2130 CH N CH CH N 1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 2131 CH N CH CH N 1-(2-pyridyl)-3-pyrrolidinyl 2132 CH N CH CH N 1-(3-pyridyl)-3-pyrrolidinyl 2133 CH N CH CH N 1-(4-pyridyl)-3-pyrrolidinyl 2134 CH N CH CH N 1-(2-pyrimidinyl)-3-pyrrolidinyl 2135 CH N CH CH N 5-oxo-1-phenyl-3-pyrrolidinyl 2136 CH N CH CH N 1-phenyl-3-piperidyl 2137 CH N CH CH N 1-(2-fluorophenyl)-3-piperidyl 2138 CH N CH CH N 1-(3-fluorophenyl)-3-piperidyl 2139 CH N CH CH N 1-(4-fluorophenyl)-3-piperidyl 2140 CH N CH CH N 1-(2-chlorophenyl)-3-piperidyl 2141 CH N CH CH N 1-(3-chlorophenyl)-3-piperidyl 2142 CH N CH CH N 1-(4-chlorophenyl)-3-piperidyl 2143 CH N CH CH N 1-(2-methylphenyl)-3-piperidyl 2144 CH N CH CH N 1-(3-methylphenyl)-3-piperidyl 2145 CH N CH CH N 1-(4-methylphenyl)-3-piperidyl 2146 CH N CH CH N 1-(2-methoxyphenyl)-3-piperidyl 2147 CH N CH CH N 1-(3-methoxyphenyl)-3-piperidyl 2148 CH N CH CH N 1-(4-methoxyphenyl)-3-piperidyl 2149 CH N CH CH N 1-(2-trifluoromethylphenyl)-3- piperidyl 2150 CH N CH CH N 1-(3-trifluoromethylphenyl)-3- piperidyl 2151 CH N CH CH N 1-(4-trifluoromethylphenyl)-3- piperidyl 2152 CH N CH CH N 1-(3,5-difluorophenyl)-3-piperidyl 2153 CH N CH CH N 1-(2-difluoromethoxyphenyl)-3- piperidyl 2154 CH N CH CH N 1-(3-difluoromethoxyphenyl)-3- piperidyl 2155 CH N CH CH N 1-(4-difluoromethoxyphenyl)-3- piperidyl 2156 CH N CH CH N 1-(2-pyridyl)-3-piperidyl 2157 CH N CH CH N 1-(3-pyridyl)-3-piperidyl 2158 CH N CH CH N 1-(4-pyridyl)-3-piperidyl 2159 CH N CH CH N 1-phenyl-4-piperidyl 2160 CH N CH CH N 1-(2-fluorophenyl)-4-piperidyl 2161 CH N CH CH N 1-(3-fluorophenyl)-4-piperidyl 2162 CH N CH CH N 1-(4-fluorophenyl)-4-piperidyl 2163 CH N CH CH N 1-(2-chlorophenyl)-4-piperidyl 2164 CH N CH CH N 1-(3-chlorophenyl)-4-piperidyl 2165 CH N CH CH N 1-(4-chlorophenyl)-4-piperidyl 2166 CH N CH CH N 1-(2-methylphenyl)-4-piperidyl 2167 CH N CH CH N 1-(3-methylphenyl)-4-piperidyl 2168 CH N CH CH N 1-(4-methylphenyl)-4-piperidyl 2169 CH N CH CH N 1-(2-methoxyphenyl)-4-piperidyl 2170 CH N CH CH N 1-(3-methoxyphenyl)-4-piperidyl 2171 CH N CH CH N 1-(4-methoxyphenyl)-4-piperidyl 2172 CH N CH CH N 1-(2-trifluoromethylphenyl)-4- piperidyl 2173 CH N CH CH N 1-(3-trifluoromethylphenyl)-4- piperidyl 2174 CH N CH CH N 1-(4-trifluoromethylphenyl)-4- piperidyl 2175 CH N CH CH N 1-(3,5-difluorophenyl)-4-piperidyl 2176 CH N CH CH N 1-(2-difluoromethoxyphenyl)-4- piperidyl 2177 CH N CH CH N 1-(3-difluoromethoxyphenyl)-4- piperidyl 2178 CH N CH CH N 1-(4-difluoromethoxyphenyl)-4- piperidyl 2179 CH N CH CH N 1-(2-pyridyl)-4-piperidyl 2180 CH N CH CH N 1-(3-pyridyl)-4-piperidyl 2181 CH N CH CH N 1-(4-pyridyl)-4-piperidyl 2182 CH N CH CH N 3-hydroxymethyl-1-phenyl-4- piperidyl 2183 CH N CH CH N 3-methoxycarbonyl-1-phenyl-4- piperidyl 2184 CH N CH CH N 3-ethoxycarbonyl-1-phenyl-4- piperidyl 2185 CH N CH CH N 3-isopropoxycarbonyl-1-phenyl-4- piperidyl 2186 CH N CH CH N 4-phenylcyclohexyl 2187 CH N CH CH N 4-(2-fluorophenyl)cyclohexyl 2188 CH N CH CH N 4-(3-fluorophenyl)cyclohexyl 2189 CH N CH CH N 4-(4-fluorophenyl)cyclohexyl 2190 CH N CH CH N 4-(2-chlorophenyl)cyclohexyl 2191 CH N CH CH N 4-(3-chlorophenyl)cyclohexyl 2192 CH N CH CH N 4-(4-chlorophenyl)cyclohexyl 2193 CH N CH CH N 4-(2-methylphenyl)cyclohexyl 2194 CH N CH CH N 4-(3-methylphenyl)cyclohexyl 2195 CH N CH CH N 4-(4-methylphenyl)cyclohexyl 2196 CH N CH CH N 4-(2-methoxyphenyl)cyclohexyl 2197 CH N CH CH N 4-(3-methoxyphenyl)cyclohexyl 2198 CH N CH CH N 4-(4-methoxyphenyl)cyclohexyl 2199 CH N CH CH N 4-(2-trifluoromethylphenyl)cyclo- hexyl 2200 CH N CH CH N 4-(3-trifluoromethylphenyl)cyclo- hexyl 2201 CH N CH CH N 4-(4-trifluoromethylphenyl)cyclo- hexyl 2202 CH N CH CH N 4-(3,5-difluorophenyl)cyclohexyl 2203 CH N CH CH N 4-(3-acetylphenyl)cyclohexyl 2204 CH N CH CH N 4-(3-cyanophenyl)cyclohexyl 2205 CH N CH CH N 4-(2-difluoromethoxyphenyl)cyclo- hexyl 2206 CH N CH CH N 4-(3-difluoromethoxyphenyl)cyclo- hexyl 2207 CH N CH CH N 4-(4-difluoromethoxyphenyl)cyclo- hexyl 2208 CH N CH CH N 4-(2-pyridyl)cyclohexyl 2209 CH N CH CH N 4-(3-pyridyl)cyclohexyl 2210 CH N CH CH N 4-(4-pyridyl)cyclohexyl 2211 CH N CH CH N 4-(4-fluoro-3-pyridyl)cyclohexyl 2212 CH N CH CH N 4-(3-quinolyl)cyclohexyl 2213 CH N CH CH N 4-(3-fluorophenyl)-4-hydroxycyclo- hexyl 2214 CH N CH CH N 3-phenylcyclohexyl 2215 CH N CH CH N 3-phenylcyclopentyl 2216 CH N CH CH N 6-phenyl-3-tetrahydropyranyl 2217 CH N CH CH N 6-(3-fluorophenyl)-3- tetrahydropyranyl 2218 CH N CH CH N 2-phenylcyclopropyl 2219 CH N CH CH N 2-(2-pyridyl)cyclopropyl 2220 CH N CH CH N 2-(3-pyridyl)cyclopropyl 2221 CH N CH CH N 2-(4-pyridyl)cyclopropyl 2222 CH N CH CH N 2-(3-fluorophenyl)cyclopropyl 2223 CH N CH CH N 2-indanyl 2224 CH N CH CH N 2-tetrahydronaphthyl 2225 CH N CH CH N 6-methoxy-2-tetrahydronaphthyl 2226 CH N CH CH N benzyl 2227 CH N CH CH N phenethyl 2228 CH N CH CH N 3-phenylpropyl 2229 CH N CH CH N 4-phenylbutyl 2230 CH N CH CH N 2-methoxyphenethyl 2231 CH N CH CH N 3-methoxyphenethyl 2232 CH N CH CH N 4-methoxyphenethyl 2233 CH N CH CH N 4-fluorophenethyl 2234 CH N CH CH N 4-bromophenethyl 2235 CH N CH CH N 4-chlorophenethyl 2236 CH N CH CH N 3-trifiluoromethylphenethyl 2237 CH N CH CH N 3,4-dimethoxyphenethyl 2238 CH N CH CH N 3-propoxyphenethyl 2239 CH N CH CH N 3,5-difluorophenethyl 2240 CH N CH CH N 4-dimethylaminophenethyl 2241 CH N CH CH N 3-difluoromethoxyphenethyl 2242 CH N CH CH N 2-methylphenethyl 2243 CH N CH CH N 4-acetylphenethyl 2244 CH N CH CH N 4-dimethylamino-2-methoxyphenethyl 2245 CH N CH CH N cyclohexylethyl 2246 CH N CH CH N 2-(2-pyridyl)ethyl 2247 CH N CH CH N 2-(3-pyridyl)ethyl 2248 CH N CH CH N 2-(4-pyridyl)ethyl 2249 CH N CH CH N 2-(2-quinolyl)ethyl 2250 CH N CH CH N 2-(3-quinolyl)ethyl 2251 CH N CH CH N 2-(4-quinolyl)ethyl 2252 CH N CH CH N 2-(6-quinolyl)ethyl 2253 CH N CH CH N 2-(2-indolyl)ethyl 2254 CH N CH CH N 2-(3-indolyl)ethyl 2255 CH N CH CH N 2-(7-aza-3-indolyl)ethyl 2256 CH N CH CH N 2-(benzimidazolyl)ethyl 2257 CH N CH CH N 2-(benzoxazolyl)ethyl 2258 CH N CH CH N 2-(benzothiazolyl)ethyl 2259 CH N CH CH N 2-(1-naphthyl)ethyl 2260 CH N CH CH N 2-(2-naphthyl)ethyl 2261 CH N CH CH N 1-(hydroxymethyl)-2-phenylethyl 2262 CH N CH CH N 1-(methoxycarbonyl)-2-phenylethyl 2263 CH N CH CH N 1-(ethoxycarbonyl)-2-phenylethyl 2264 CH N CH CH N 1-carboxy-2-phenylethyl 2265 CH N CH CH N 1-(benzyloxycarbonyl)-2-phenyl- ethyl 2266 CH N CH CH N 1-(phenoxymethyl)-2-phenylethyl 2267 CH N CH CH N 1-(benzyloxymethyl)-2-phenylethyl 2268 CH N CH CH N 1-(benzylcarbamoyl)-2-phenylethyl 2269 CH N CH CH N 1-(N-methylbenzylcarbamoyl)-2- phenylethyl 2270 CH N CH CH N 1-(phenylcarbamoyl)-2-phenylethyl 2271 CH N CH CH N 1-(N-methylphenylcarbamoyl)-2- phenylethyl 2272 CH N CH CH N 1-(N-benzylaminomethyl)-2- phenylethyl 2273 CH N CH CH N 1-(N-benzyl-N-methylaminomethyl)- 2-phenylethyl 2274 CH N CH CH N 1-(anilinomethyl)-2-phenylethyl 2275 CH N CH CH N 1-(N-methylanilinomethyl)-2- phenylethyl 2276 CH N CH CH N 1-(N-methylaminomethyl)-2- phenylethyl 2277 CH N CH CH N 1-(N-ethylaminomethyl)-2- phenylethyl 2278 CH N CH CH N 1-(N-isobutylaminomethyl)-2- phenylethyl 2279 CH N CH CH N 1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 2280 CH N CH CH N 1-(aminomethyl)-2-phenylethyl 2281 CH N CH CH N 1-benzyl-2-(2-pyridylmethyl- amino)ethyl 2282 CH N CH CH N 1-benzyl-2-(3-pyridylmethyl- amino)ethyl 2283 CH N CH CH N 1-benzyl-2-(4-pyridylmethyl- amino)ethyl 2284 CH N CH CH N 2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 2285 CH N CH CH N 2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 2286 CH N CH CH N 2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 2287 CH N CH CH N 2-hydroxy-2-phenylethyl 2288 CH N CH CH N benzoylmethyl 2289 CH N CH CH N 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 2290 CH N CH CH N 1-(benzyloxycarbonyl)-2- cyclohexylethyl 2291 CH N CH CH N 1-(phenoxymethyl)-2-(3- indolyl)ethyl 2292 CH N CH CH N 2-(2-methoxyphenoxy)ethyl 2293 CH N CH CH N 1-(benzylcarbamoyl)-2- cyclohexylethyl 2294 CH N CH CH N 1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 2295 CH N CH CH N 1-(phenylcarbamoyl)-2- cyclohexylethyl 2296 CH N CH CH N 1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 2297 CH N CH CH N 1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 2298 CH N CH CH N 1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 2299 CH N CH CH N 1-(benzylcarbamoyl)-2-(4- pyridyl)ethyl 2300 CH N CH CH N 1-(4-pyridylmethylcarbamoyl)-2- (4-fluorophenyl)ethyl 2301 CH N CH CH N 1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 2302 CH N CH CH N 1-(benzyloxymethyl)-2-(2- indolyl)ethyl 2303 CH N CH CH N 1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 2304 CH N CH CH N 1-(N-methylbenzylcarbamoyl)-2- (3-pyridyl)ethyl 2305 CH N CH CH N 2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 2306 CH N CH CH N 2-hydroxy-2-(2-quinolyl)ethyl 2307 CH N CH CH N 2-hydroxy-2-(3-quinolyl)ethyl 2308 CH N CH CH N 2-hydroxy-2-(4-quinolyl)ethyl 2309 CH N CH CH N 2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 2310 CH N CH CH N 1-carboxy-2-cyclohexylethyl 2311 CH N CH CH N 2-hydroxy-2-(6-quinolyl)ethyl 2312 CH N CH CH N 2-(benzylamino)-2-phenylethyl 2313 CH N CH CH N 2-amino-2-(2-naphthyl)propyl 2314 CH N CH CH N 2-(phenylamino)ethyl 2315 CH N CH CH N diphenylmethyl 2316 CH N CH CH N 2,2-diphenylethyl 2317 CH N CH CH N 2-phenyl-2-(2-pyridyl)ethyl 2318 CH N CH CH N 2-phenyl-2-(3-pyridyl)ethyl 2319 CH N CH CH N 2-phenyl-2-(4-pyridyl)ethyl 2320 CH N CH CH N 2-phenoxy-2-phenylethyl 2321 CH N CH CH N 2-(benzyloxy)-2-phenylethyl 2322 CH CH N CH CH 1-phenyl-3-pyrrolidinyl 2323 CH CH N CH CH 1-(2-fluorophenyl)-3-pyrrolidinyl 2324 CH CH N CH CH 1-(3-fluorophenyl)-3-pyrrolidinyl 2325 CH CH N CH CH 1-(4-fluorophenyl)-3-pyrrolidinyl 2326 CH CH N CH CH 1-(2-chlorophenyl)-3-pyrrolidinyl 2327 CH CH N CH CH 1-(3-chlorophenyl)-3-pyrrolidinyl 2328 CH CH N CH CH 1-(4-chlorophenyl)-3-pyrrolidinyl 2329 CH CH N CH CH 1-(2-methylphenyl)-3-pyrrolidinyl 2330 CH CH N CH CH 1-(3-methylphenyl)-3-pyrrolidinyl 2331 CH CH N CH CH 1-(4-methylphenyl)-3-pyrrolidinyl 2332 CH CH N CH CH 1-(2-methoxyphenyl)-3-pyrrolidinyl 2333 CH CH N CH CH 1-(3-methoxyphenyl)-3-pyrrolidinyl 2334 CH CH N CH CH 1-(4-methoxyphenyl)-3- pyrrolidinyl 2335 CH CH N CH CH 1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 2336 CH CH N CH CH 1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 2337 CH CH N CH CH 1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 2338 CH CH N CH CH 1-(3,5-difluorophenyl)-3- pyrrolidinyl 2339 CH CH N CH CH 1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 2340 CH CH N CH CH 1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 2341 CH CH N CH CH 1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 2342 CH CH N CH CH 1-(2-pyridyl)-3-pyrrolidinyl 2343 CH CH N CH CH 1-(3-pyridyl)-3-pyrrolidinyl 2344 CH CH N CH CH 1-(4-pyridyl)-3-pyrrolidinyl 2345 CH CH N CH CH 1-(2-pyrimidinyl)-3-pyrrolidinyl 2346 CH CH N CH CH 5-oxo-1-phenyl-3-pyrrolidinyl 2347 CH CH N CH CH 1-phenyl-3-piperidyl 2348 CH CH N CH CH 1-(2-fluorophenyl)-3-piperidyl 2349 CH CH N CH CH 1-(3-fluorophenyl)-3-piperidyl 2350 CH CH N CH CH 1-(4-fluorophenyl)-3-piperidyl 2351 CH CH N CH CH 1-(2-chlorophenyl)-3-piperidyl 2352 CH CH N CH CH 1-(3-chlorophenyl)-3-piperidyl 2353 CH CH N CH CH 1-(4-chlorophenyl)-3-piperidyl 2354 CH CH N CH CH 1-(2-methylphenyl)-3-piperidyl 2355 CH CH N CH CH 1-(3-methylphenyl)-3-piperidyl 2356 CH CH N CH CH 1-(4-methylphenyl)-3-piperidyl 2357 CH CH N CH CH 1-(2-methoxyphenyl)-3-piperidyl 2358 CH CH N CH CH 1-(3-methoxyphenyl)-3-piperidyl 2359 CH CH N CH CH 1-(4-methoxyphenyl)-3-piperidyl 2360 CH CH N CH CH 1-(2-trifluoromethylphenyl)-3- piperidyl 2361 CH CH N CH CH 1-(3-trifluoromethylphenyl)-3- piperidyl 2362 CH CH N CH CH 1-(4-trifluoromethylphenyl)-3- piperidyl 2363 CH CH N CH CH 1-(3,5-difluorophenyl)-3-piperidyl 2364 CH CH N CH CH 1-(2-difluoromethoxyphenyl)-3- piperidyl 2365 CH CH N CH CH 1-(3-difluoromethoxyphenyl)-3- piperidyl 2366 CH CH N CH CH 1-(4-difluoromethoxyphenyl)-3- piperidyl 2367 CH CH N CH CH 1-(2-pyridyl)-3-piperidyl 2368 CH CH N CH CH 1-(3-pyridyl)-3-piperidyl 2369 CH CH N CH CH 1-(4-pyridyl)-3-piperidyl 2370 CH CH N CH CH 1-phenyl-4-piperidyl 2371 CH CH N CH CH 1-(2-fluorophenyl)-4-piperidyl 2372 CH CH N CH CH 1-(3-fluorophenyl)-4-piperidyl 2373 CH CH N CH CH 1-(4-fluorophenyl)-4-piperidyl 2374 CH CH N CH CH 1-(2-chlorophenyl)-4-piperidyl 2375 CH CH N CH CH 1-(3-chlorophenyl)-4-piperidyl 2376 CH CH N CH CH 1-(4-chlorophenyl)-4-piperidyl 2377 CH CH N CH CH 1-(2-methylphenyl)-4-piperidyl 2378 CH CH N CH CH 1-(3-methylphenyl)-4-piperidyl 2379 CH CH N CH CH 1-(4-methylphenyl)-4-piperidyl 2380 CH CH N CH CH 1-(2-methoxyphenyl)-4-piperidyl 2381 CH CH N CH CH 1-(3-methoxyphenyl)-4-piperidyl 2382 CH CH N CH CH 1-(4-methoxyphenyl)-4-piperidyl 2383 CH CH N CH CH 1-(2-trifluoromethylphenyl)-4- piperidyl 2384 CH CH N CH CH 1-(3-trifluoromethylphenyl)-4- piperidyl 2385 CH CH N CH CH 1-(4-trifluoromethylphenyl)-4- piperidyl 2386 CH CH N CH CH 1-(3,5-difluorophenyl)-4-piperidyl 2387 CH CH N CH CH 1-(2-difluoromethoxyphenyl)-4- piperidyl 2388 CH CH N CH CH 1-(3-difluoromethoxyphenyl)-4- piperidyl 2389 CH CH N CH CH 1-(4-difluoromethoxyphenyl)-4- piperidyl 2390 CH CH N CH CH 1-(2-pyridyl)-4-piperidyl 2391 CH CH N CH CH 1-(3-pyridyl)-4-piperidyl 2392 CH CH N CH CH 1-(4-pyridyl)-4-piperidyl 2393 CH CH N CH CH 3-hydroxymethyl-1-phenyl-4- piperidyl 2394 CH CH N CH CH 3-methoxycarbonyl-1-phenyl-4- piperidyl 2395 CH CH N CH CH 3-ethoxycarbonyl-1-phenyl-4- piperidyl 2396 CH CH N CH CH 3-isopropoxycarbonyl-1-phenyl-4- piperidyl 2397 CH CH N CH CH 4-phenylcyclohexyl 2398 CH CH N CH CH 4-(2-fluorophenyl)cyclohexyl 2399 CH CH N CH CH 4-(3-fluorophenyl)cyclohexyl 2400 CH CH N CH CH 4-(4-fluorophenyl)cyclohexyl 2401 CH CH N CH CH 4-(2-chlorophenyl)cyclohexyl 2402 CH CH N CH CH 4-(3-chlorophenyl)cyclohexyl 2403 CH CH N CH CH 4-(4-chlorophenyl)cyclohexyl 2404 CH CH N CH CH 4-(2-methylphenyl)cyclohexyl 2405 CH CH N CH CH 4-(3-methylphenyl)cyclohexyl 2406 CH CH N CH CH 4-(4-methylphenyl)cyclohexyl 2407 CH CH N CH CH 4-(2-methoxyphenyl)cyclohexyl 2408 CH CH N CH CH 4-(3-methoxyphenyl)cyclohexyl 2409 CH CH N CH CH 4-(4-methoxyphenyl)cyclohexyl 2410 CH CH N CH CH 4-(2-trifluoromethylphenyl)cyclo- hexyl 2411 CH CH N CH CH 4-(3-trifluoromethylphenyl)cyclo- hexyl 2412 CH CH N CH CH 4-(4-trifluoromethylphenyl)cyclo- hexyl 2413 CH CH N CH CH 4-(3,5-difluorophenyl)cyclohexyl 2414 CH CH N CH CH 4-(3-acetylphenyl)cyclohexyl 2415 CH CH N CH CH 4-(3-cyanophenyl)cyclohexyl 2416 CH CH N CH CH 4-(2-difluoromethoxyphenyl)cyclo- hexyl 2417 CH CH N CH CH 4-(3-difluoromethoxyphenyl)cyclo- hexyl 2418 CH CH N CH CH 4-(4-difluoromethoxyphenyl)cyclo- hexyl 2419 CH CH N CH CH 4-(2-pyridyl)cyclohexyl 2420 CH CH N CH CH 4-(3-pyridyl)cyclohexyl 2421 CH CH N CH CH 4-(4-pyridyl)cyclohexyl 2422 CH CH N CH CH 4-(4-fluoro-3-pyridyl)cyclohexyl 2423 CH CH N CH CH 4-(3-quinolyl)cyclohexyl 2424 CH CH N CH CH 4-(3-fluorophenyl)-4-hydroxy- cyclohexyl 2425 CH CH N CH CH 3-phenylcyclohexyl 2426 CH CH N CH CH 3-phenylcyclopentyl 2427 CH CH N CH CH 6-phenyl-3-tetrhydropyranyl 2428 CH CH N CH CH 6-(3-fluorophenyl)-3-tetrhydro- pyranyl 2429 CH CH N CH CH 2-phenylcyclopropyl 2430 CH CH N CH CH 2-(2-pyridyl)cyclopropyl 2431 CH CH N CH CH 2-(3-pyridyl)cyclopropyl 2432 CH CH N CH CH 2-(4-pyridyl)cyclopropyl 2433 CH CH N CH CH 2-(3-fluorophenyl)cyclopropyl 2434 CH CH N CH CH 2-indanyl 2435 CH CH N CH CH 2-tetrahydronaphthyl 2436 CH CH N CH CH 6-methoxy-2-tetrahydronaphthyl 2437 CH CH N CH CH benzyl 2438 CH CH N CH CH phenethyl 2439 CH CH N CH CH 3-phenylpropyl 2440 CH CH N CH CH 4-phenylbutyl 2441 CH CH N CH CH 2-methoxyphenethyl 2442 CH CH N CH CH 3-methoxyphenethyl 2443 CH CH N CH CH 4-methoxyphenethyl 2444 CH CH N CH CH 4-fluorophenethyl 2445 CH CH N CH CH 4-bromophenethyl 2446 CH CH N CH CH 4-chlorophenethyl 2447 CH CH N CH CH 3-trifluoromethylphenethyl 2448 CH CH N CH CH 3,4-dimethoxyphenethyl 2449 CH CH N CH CH 3-propoxyphenethyl 2450 CH CH N CH CH 3,5-difluorophenethyl 2451 CH CH N CH CH 4-dimethylaminophenethyl 2452 CH CH N CH CH 3-difluoromethoxyphenethyl 2453 CH CH N CH CH 2-methylphenethyl 2454 CH CH N CH CH 4-acetylphenethyl 2455 CH CH N CH CH 4-dimethylamino-2-methoxyphenethyl 2456 CH CH N CH CH cyclohexylethyl 2457 CH CH N CH CH 2-(2-pyridyl)ethyl 2458 CH CH N CH CH 2-(3-pyridyl)ethyl 2459 CH CH N CH CH 2-(4-pyridyl)ethyl 2460 CH CH N CH CH 2-(2-quinolyl)ethyl 2461 CH CH N CH CH 2-(3-quinolyl)ethyl 2462 CH CH N CH CH 2-(4-quinolyl)ethyl 2463 CH CH N CH CH 2-(6-quinolyl)ethyl 2464 CH CH N CH CH 2-(2-indolyl)ethyl 2465 CH CH N CH CH 2-(3-indolyl)ethyl 2466 CH CH N CH CH 2-(7-aza-3-indolyl)ethyl 2467 CH CH N CH CH 2-(benzimidazolyl)ethyl 2468 CH CH N CH CH 2-(benzoxazolyl)ethyl 2469 CH CH N CH CH 2-(benzothiazolyl)ethyl 2470 CH CH N CH CH 2-(1-naphthyl)ethyl 2471 CH CH N CH CH 2-(2-naphthyl)ethyl 2472 CH CH N CH CH 1-(hydroxymethyl)-2-phenylethyl 2473 CH CH N CH CH 1-(methoxycarbonyl)-2-phenylethyl 2474 CH CH N CH CH 1-(ethoxycarbonyl)-2-phenylethyl 2475 CH CH N CH CH 1-carboxy-2-phenylethyl 2476 CH CH N CH CH 1-(benzyloxycarbonyl)-2-phenyl- ethyl 2477 CH CH N CH CH 1-(phenoxymethyl)-2-phenylethyl 2478 CH CH N CH CH 1-(benzyloxymethyl)-2-phenylethyl 2479 CH CH N CH CH 1-(benzylcarbamoyl)-2-phenylethyl 2480 CH CH N CH CH 1-(N-methylbenzylcarbamoyl)-2- phenylethyl 2481 CH CH N CH CH 1-(phenylcarbamoyl)-2-phenylethyl 2482 CH CH N CH CH 1-(N-methylphenylcarbamoyl)-2- phenylethyl 2483 CH CH N CH CH 1-(N-benzylaminomethyl)-2-phenyl- ethyl 2484 CH CH N CH CH 1-(N-benzyl-N-methylaminomethyl)- 2-phenylethyl 2485 CH CH N CH CH 1-(anilinomethyl)-2-phenylethyl 2486 CH CH N CH CH 1-(N-methylanilinomethyl)-2- phenylethyl 2487 CH CH N CH CH 1-(N-methylaminomethyl)-2- phenylethyl 2488 CH CH N CH CH 1-(N-ethylaminomethyl)-2- phenylethyl 2489 CH CH N CH CH 1-(N-isobutylaxninomethyl)-2- phenylethyl 2490 CH CH N CH CH 1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 2491 CH CH N CH CH 1-(aminomethyl)-2-phenylethyl 2492 CH CH N CH CH 1-benzyl-2-(2-pyridylmethyl- amino)ethyl 2493 CH CH N CH CH 1-benzyl-2-(3-pyridylmethyl- amino)ethyl 2494 CH CH N CH CH 1-benzyl-2-(4-pyridylmethyl- amino)ethyl 2495 CH CH N CH CH 2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 2496 CH CH N CH CH 2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 2497 CH CH N CH CH 2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 2498 CH CH N CH CH 2-hydroxy-2-phenylethyl 2499 CH CH N CH CH benzoylmethyl 2500 CH CH N CH CH 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 2501 CH CH N CH CH 1-(benzyloxycarbonyl)-2-cyclo- hexylethyl 2502 CH CH N CH CH 1-(phenoxymethyl)-2-(3- indolyl)ethyl 2503 CH CH N CH CH 2-(2-methoxyphenoxy)ethyl 2504 CH CH N CH CH 1-(benzylcarbamoyl)-2-cyclohexyl- ethyl 2505 CH CH N CH CH 1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 2506 CH CH N CH CH 1-(phenylcarbamoyl)-2-cyclohexyl- ethyl 2507 CH CH N CH CH 1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 2508 CH CH N CH CH 1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 2509 CH CH N CH CH 1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 2510 CH CH N CH CH 1-(benzylcarbamoyl)-2-(4- pyridyl)ethyl 2511 CH CH N CH CH 1-(4-pyridylmethylcarbamoyl)-2-(4- fluorophenyl)ethyl 2512 CH CH N CH CH 1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 2513 CH CH N CH CH 1-(benzyloxymethyl)-2-(2- indolyl)ethyl 2514 CH CH N CH CH 1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 2515 CH CH N CH CH 1-(N-methylbenzylcarbanioyl)-2- (3-pyridyl)ethyl 2516 CH CH N CH CH 2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 2517 CH CH N CH CH 2-hydroxy-2-(2-quinolyl)ethyl 2518 CH CH N CH CH 2-hydroxy-2-(3-quinolyl)ethyl 2519 CH CH N CH CH 2-hydroxy-2-(4-quinolyl)ethyl 2520 CH CH N CH CH 2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 2521 CH CH N CH CH 1-carboxy-2-cyclohexylethyl 2522 CH CH N CH CH 2-hydroxy-2-(6-quinolyl)ethyl 2523 CH CH N CH CH 2-(benzylamino)-2-phenylethyl 2524 CH CH N CH CH 2-amino-2-(2-naphthyl)propyl 2525 CH CH N CH CH 2-(phenylamino)ethyl 2526 CH CH N CH CH diphenylmethyl 2527 CH CH N CH CH 2,2-diphenylethyl 2528 CH CH N CH CH 2-phenyl-2-(2-pyridyl)ethyl 2529 CH CH N CH CH 2-phenyl-2-(3-pyridyl)ethyl 2530 CH CH N CH CH 2-phenyl-2-(4-pyridyl)ethyl 2531 CH CH N CH CH 2-phenoxy-2-phenylethyl 2532 CH CH N CH CH 2-(benzyloxy)-2-phenylethyl 2533 CH CH N CH N 1-phenyl-3-pyrrolidinyl 2534 CH CH N CH N 1-(2-fluorophenyl)-3-pyrrolidinyl 2535 CH CH N CH N 1-(3-fluorophenyl)-3-pyrrolidinyl 2536 CH CH N CH N 1-(4-fluorophenyl)-3-pyrrolidinyl 2537 CH CH N CH N 1-(2-chlorophenyl)-3-pyrrolidinvl 2538 CH CH N CH N 1-(3-chlorophenyl)-3-pyrrolidinyl 2539 CH CH N CH N 1-(4-chlorophenyl)-3-pyrrolidinyl 2540 CH CH N CH N 1-(2-methylphenyl)-3-pyrrolidinyl 2541 CH CH N CH N 1-(3-methylphenyl)-3-pyrrolidinyl 2542 CH CH N CH N 1-(4-methylphenyl)-3-pyrrolidinyl 2543 CH CH N CH N 1-(2-methoxyphenyl)-3-pyrrolidinyl 2544 CH CH N CH N 1-(3-methoxyphenyl)-3-pyrrolidinyl 2545 CH CH N CH N 1-(4-methoxyphenyl)-3-pyrrolidinyl 2546 CH CH N CH N 1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 2547 CH CH N CH N 1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 2548 CH CH N CH N 1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 2549 CH CH N CH N 1-(3,5-diflurophenyl)-3- pyrrolidinyl 2550 CH CH N CH N 1-(2-difluromethoxyphenyl)-3- pyrrolidinyl 2551 CH CH N CH N 1-(3-difluromethoxyphenyl)-3- pyrrolidinyl 2552 CH CH N CH N 1-(4-difluromethoxyphenyl)-3- pyrrolidinyl 2553 CH CH N CH N 1-(2-pyridyl)-3-pyrrolidinyl 2554 CH CH N CH N 1-(3-pyridyl)-3-pyrrolidinyl 2555 CH CH N CH N 1-(4-pyridyl)-3-pyrrolidinyl 2556 CH CH N CH N 1-(2-pyrimidinyl)-3-pyrrolidinyl 2557 CH CH N CH N 5-oxo-1-phenyl-3-pyrrolidinyl 2558 CH CH N CH N 1-phenyl-3-piperidyl 2559 CH CH N CH N 1-(2-fluorophenyl)-3-piperidyl 2560 CH CH N CH N 1-(3-fluorophenyl)-3-piperidyl 2561 CH CH N CH N 1-(4-fluorophenyl)-3-piperidyl 2562 CH CH N CH N 1-(2-chlorophenyl)-3-piperidyl 2563 CH CH N CH N 1-(3-chlorophenyl)-3-piperidyl 2564 CH CH N CH N 1-(4-chlorophenyl)-3-piperidyl 2565 CH CH N CH N 1-(2-methylphenyl)-3-piperidyl 2566 CH CH N CH N 1-(3-methylphenyl)-3-piperidyl 2567 CH CH N CH N 1-(4-methylphenyl)-3-piperidyl 2568 CH CH N CH N 1-(2-methoxyphenyl)-3-piperidyl 2569 CH CH N CH N 1-(3-methoxyphenyl)-3-piperidyl 2570 CH CH N CH N 1-(4-methoxyphenyl4-3-piperidyl 2571 CH CH N CH N 1-(2-trifluoromethylphenyl)-3- piperidyl 2572 CH CH N CH N 1-(3-trifluoromethylphenyl)-3- piperidyl 2573 CH CH N CH N 1-(4-trifluoromethylphenyl)-3- piperidyl 2574 CH CH N CH N 1-(3,5-difluorophenyl)-3-piperidyl 2575 CH CH N CH N 1-(2-difluoromethoxyphenyl)-3- piperidyl 2576 CH CH N CH N 1-(3-difluoromethoxyphenyl)-3- piperidyl 2577 CH CH N CH N 1-(4-difluoromethoxyphenyl)-3- piperidyl 2578 CH CH N CH N 1-(2-pyridyl)-3-piperidyl 2579 CH CH N CH N 1-(3-pyridyl)-3-piperidyl 2580 CH CH N CH N 1-(4-pyridyl)-3-piperidyl 2581 CH CH N CH N 1-phenyl-4-piperidyl 2582 CH CH N CH N 1-(2-fluorophenyl)-4-piperidyl 2583 CH CH N CH N 1-(3-fluorophenyl)-4-piperidyl 2584 CH CH N CH N 1-(4-fluorophenyl)-4-piperidyl 2585 CH CH N CH N 1-(2-chlorophenyl)-4-piperidyl 2586 CH CH N CH N 1-(3-chlorophenyl)-4-piperidyl 2587 CH CH N CH N 1-(4-chlorophenyl)-4-piperidyl 2588 CH CH N CH N 1-(2-methylphenyl)-4-piperidyl 2589 CH CH N CH N 1-(3-methylphenyl)-4-piperidyl 2590 CH CH N CH N 1-(4-methylphenyl)-4-piperidyl 2591 CH CH N CH N 1-(2-methoxyphenyl)-4-piperidyl 2592 CH CH N CH N 1-(3-methoxyphenyl)-4-piperidyl 2593 CH CH N CH N 1-(4-methoxyphenyl)-4-piperidyl 2594 CH CH N CH N 1-(2-trifluoromethylphenyl)-4- piperidyl 2595 CH CH N CH N 1-(3-trifluoromethylphenyl)-4- piperidyl 2596 CH CH N CH N 1-(4-trifluoromethylphenyl)-4- piperidyl 2597 CH CH N CH N 1-(3,5-difluorophenyl)-4- piperidyl 2598 CH CH N CH N 1-(2-difluoromethoxyphenyl)-4- piperidyl 2599 CH CH N CH N 1-(3-difluoromethoxyphenyl)-4- piperidyl 2600 CH CH N CH N 1-(4-difluoromethoxyphenyl)-4- piperidyl 2601 CH CH N CH N 1-(2-pyridyl)-4-piperidyl 2602 CH CH N CH N 1-(3-pyridyl)-4-piperidyl 2603 CH CH N CH N 1-(4-pyridyl)-4-piperidyl 2604 CH CH N CH N 3-hydroxymethyl-1-phenyl-4- piperidyl 2605 CH CH N CH N 3-methoxycarbonyl-1-phenyl-4- piperidyl 2606 CH CH N CH N 3-ethoxycarbonyl-1-phenyl-4- piperidyl 2607 CH CH N CH N 3-isopropoxycarbonyl-1-phenyl-4- piperidyl 2608 CH CH N CH N 4-phenylcyclohexyl 2609 CH CH N CH N 4-(2-fluorophenyl)cyclohexyl 2610 CH CH N CH N 4-(3-fluorophenyl)cyclohexyl 2611 CH CH N CH N 4-(4-fluorophenyl)cyclohexyl 2612 CH CH N CH N 4-(2-chlorophenyl)cyclohexyl 2613 CH CH N CH N 4-(3-chlorophenyl)cyclohexyl 2614 CH CH N CH N 4-(4-chlorophenyl)cyclohexyl 2615 CH CH N CH N 4-(2-methylphenyl)cyclohexyl 2616 CH CH N CH N 4-(3-methylphenyl)cyclohexyl 2617 CH CH N CH N 4-(4-methylphenyl)cyclohexyl 2618 CH CH N CH N 4-(2-methoxyphenyl)cyclohexyl 2619 CH CH N CH N 4-(3-methoxyphenyl)cyclohexyl 2620 CH CH N CH N 4-(4-methoxyphenyl)cyclohexyl 2621 CH CH N CH N 4-(2-trifluoromethylphenyl)cyclo- hexyl 2622 CH CH N CH N 4-(3-trifluoromethylphenyl)cyclo- hexyl 2623 CH CH N CH N 4-(4-trifluoromethylphenyl)cyclo- hexyl 2624 CH CH N CH N 4-(3,5-difluorophenyl)cyclohexyl 2625 CH CH N CH N 4-(3-acetylphenyl)cyclohexyl 2626 CH CH N CH N 4-(3-cyanophenyl)cyclohexyl 2627 CH CH N CH N 4-(2-difluoromethoxyphenyl)cyclo- hexyl 2628 CH CH N CH N 4-(3-difluoromethoxyphenyl)cyclo- hexyl 2629 CH CH N CH N 4-(4-difluoromethoxyphenyl)cyclo- hexyl 2630 CH CH N CH N 4-(2-pyridyl)cyclohexyl 2631 CH CH N CH N 4-(3-pyridyl)cyclohexyl 2632 CH CH N CH N 4-(4-pyridyl)cyclohexyl 2633 CH CH N CH N 4-(4-fluoro-3-pyridyl)cyclohexyl 2634 CH CH N CH N 4-(3-quinolyl)cyclohexyl 2635 CH CH N CH N 4-(3-fluorophenyl)-4-hydroxy- cyclohexyl 2636 CH CH N CH N 3-phenylcyclohexyl 2637 CH CH N CH N 3-phenylcyclopentyl 2638 CH CH N CH N 6-phenyl-3-tetrahydropyranyl 2639 CH CH N CH N 6-(3-fluorophenyl)-3-tetrahydro- pyranyl 2640 CH CH N CH N 2-phenylcyclopropyl 2641 CH CH N CH N 2-(2-pyridyl)cyclopropyl 2642 CH CH N CH N 2-(3-pyridyl)cyclopropyl 2643 CH CH N CH N 2-(4-pyridyl)cyclopropyl 2644 CH CH N CH N 2-(3-fluorophenyl)cyclopropyl 2645 CH CH N CH N 2-indanyl 2646 CH CH N CH N 2-tetrahydronaphthyl 2647 CH CH N CH N 6-methoxy-2-tetrahydronaphthyl 2648 CH CH N CH N benzyl 2649 CH CH N CH N phenethyl 2650 CH CH N CH N 3-phenylpropyl 2651 CH CH N CH N 4-phenylbutyl 2652 CH CH N CH N 2-methoxyphenethyl 2653 CH CH N CH N 3-methoxyphenethyl 2654 CH CH N CH N 4-methoxyphenethyl 2655 CH CH N CH N 4-fluorophenethyl 2656 CH CH N CH N 4-bromophenethyl 2657 CH CH N CH N 4-chlorophenethyl 2658 CH CH N CH N 3-trifluoromethylphenethyl 2659 CH CH N CH N 3,4-dimethoxyphenethyl 2660 CH CH N CH N 3-propoxyphenethyl 2661 CH CH N CH N 3,5-difluorophenethyl 2662 CH CH N CH N 4-dimethylaminophenethyl 2663 CH CH N CH N 3-difluoromethoxyphenethyl 2664 CH CH N CH N 2-methylphenethyl 2665 CH CH N CH N 4-acetylphenethyl 2666 CH CH N CH N 4-dimethylamino-2-methoxyphenethyl 2667 CH CH N CH N cyclohexylethyl 2668 CH CH N CH N 2-(2-pyridyl)ethyl 2669 CH CH N CH N 2-(3-pyridyl)ethyl 2670 CH CH N CH N 2-(4-pyridyl)ethyl 2671 CH CH N CH N 2-(2-quinolyl)ethyl 2672 CH CH N CH N 2-(3-quinolyl)ethyl 2673 CH CH N CH N 2-(4-quinolyl)ethyl 2674 CH CH N CH N 2-(6-quinolyl)ethyl 2675 CH CH N CH N 2-(2-indolyl)ethyl 2676 CH CH N CH N 2-(3-indolyl)ethyl 2677 CH CH N CH N 2-(7-aza-3-indolyl)ethyl 2678 CH CH N CH N 2-(benzimidazolyl)ethyl 2679 CH CH N CH N 2-(benzoxazolyl)ethyl 2680 CH CH N CH N 2-(benzothiazolyl)ethyl 2681 CH CH N CH N 2-(1-naphthyl)ethyl 2682 CH CH N CH N 2-(2-naphthyl)ethyl 2683 CH CH N CH N 1-(hydroxymethyl)-2-phenylethyl 2684 CH CH N CH N 1-(methoxycarbonyl)-2-phenylethyl 2685 CH CH N CH N 1-(ethoxycarbonyl)-2-phenylethyl 2686 CH CH N CH N 1-carboxy-2-phenylethyl 2687 CH CH N CH N 1-(benzyloxycarbonyl)-2-phenyl- ethyl 2688 CH CH N CH N 1-(phenoxymethyl)-2-phenylethyl 2689 CH CH N CH N 1-(benzyloxymethyl)-2-phenylethyl 2690 CH CH N CH N 1-(benzylcarbamoyl)-2-phenylethyl 2691 CH CH N CH N 1-(N-methylbenzylcarbamoyl)-2- phenylethyl 2692 CH CH N CH N 1-(phenylcarbamoyl)-2-phenylethyl 2693 CH CH N CH N 1-(N-methylphenylcarbamoyl)-2- phenylethyl 2694 CH CH N CH N 1-(N-benzylaminomethyl)-2- phenylethyl 2695 CH CH N CH N 1-(N-benzyl-N-methylamino- methyl)-2-phenylethyl 2696 CH CH N CH N 1-(anilinomethyl)-2-phenylethyl 2697 CH CH N CH N 1-(N-methylanilinomethyl)-2- phenylethyl 2698 CH CH N CH N 1-(N-methylaminomethyl)-2- phenylethyl 2699 CH CH N CH N 1-(N-ethylaminomethyl)-2- phenylethyl 2700 CH CH N CH N 1-(N-isobutylaminomethyl)-2- phenylethyl 2701 CH CH N CH N 1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 2702 CH CH N CH N 1-(aminomethyl)-2-phenylethyl 2703 CH CH N CH N 1-benzyl-2-(2-pyridylmethyl- amino)ethyl 2704 CH CH N CH N 1-benzyl-2-(3-pyridylmethyl- amino)ethyl 2705 CH CH N CH N 1-benzyl-2-(4-pyridylmethyl- amino)ethyl 2706 CH CH N CH N 2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 2707 CH CH N CH N 2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 2708 CH CH N CH N 2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 2709 CH CH N CH N 2-hydroxy-2-phenylethyl 2710 CH CH N CH N benzoylmethyl 2711 CH CH N CH N 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 2712 CH CH N CH N 1-(benzyloxycarbonyl)-2- cyclohexylethyl 2713 CH CH N CH N 1-(phenoxymethyl)-2-(3- indolyl)ethyl 2714 CH CH N CH N 2-(2-methoxyphenoxy)ethyl 2715 CH CH N CH N 1-(benzylcarbamoyl)-2- cyclohexylethyl 2716 CH CH N CH N 1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 2717 CH CH N CH N 1-(phenylcarbamoyl)-2-cyclohexyl- ethyl 2718 CH CH N CH N 1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 2719 CH CH N CH N 1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 2720 CH CH N CH N 1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 2721 CH CH N CH N 1-(benzylcarbamoyl)-2- 4-pyridyl)ethyl 2722 CH CH N CH N 1-(4-pyridylmethylcarbamoyl)-2- (4-fluorophenyl)ethyl 2723 CH CH N CH N 1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 2724 CH CH N CH N 1-(benzyloxymethyl)-2-(2- indolyl)ethyl 2725 CH CH N CH N 1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 2726 CH CH N CH N 1-(N-methylbenzylcarbamoyl)-2- (3-pyridyl)ethyl 2727 CH CH N CH N 2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 2728 CH CH N CH N 2-hydroxy-2-(2-quinolyl)ethyl 2729 CH CH N CH N 2-hydroxy-2-(3-quinolyl)ethyl 2730 CH CH N CH N 2-hydroxy-2-(4-quinolyl)ethyl 2731 CH CH N CH N 2-hydroxy-2-(3,5-difluorophenyl) ethyl 2732 CH CH N CH N 1-carboxy-2-cyclohexylethyl 2733 CH CH N CH N 2-hydroxy-2-(6-quinolyl)ethyl 2734 CH CH N CH N 2-(benzylamino)-2-phenylethyl 2735 CH CH N CH N 2-amino-2-(2-naphthyl)propyl 2736 CH CH N CH N 2-(phenylamino)ethyl 2737 CH CH N CH N diphenylmethyl 2738 CH CH N CH N 2,2-diphenylethyl 2739 CH CH N CH N 2-phenyl-2-(2-pyridyl)ethyl 2740 CH CH N CH N 2-phenyl-2-(3-pyridyl)ethyl 2741 CH CH N CH N 2-phenyl-2-(4-pyridyl)ethyl 2742 CH CH N CH N 2-phenoxy-2-phenylethyl 2743 CH CH N CH N 2-(benzyloxy)-2-phenylethyl 2744 CH CH CH N CH 1-phenyl-3-pyrrolidinyl 2745 CH CH CH N CH 1-(2-fluorophenyl)-3-pyrrolidinyl 2746 CH CH CH N CH 1-(3-fluorophenyl)-3-pyrrolidinyl 2747 CH CH CH N CH 1-(4-fluorophenyl)-3-pyrrolidinyl 2748 CH CH CH N CH 1-(2-chlorophenyl)-3-pyrrolidinyl 2749 CH CH CH N CH 1-(3-chlorophenyl)-3-pyrrolidinyl 2750 CH CH CH N CH 1-(4-chlorophenyl)-3-pyrrolidinyl 2751 CH CH CH N CH 1-(2-methylphenyl)-3-pyrrolidinyl 2752 CH CH CH N CH 1-(3-methylphenyl)-3-pyrrolidinyl 2753 CH CH CH N CH 1-(4-methylphenyl)-3-pyrrolidinyl 2754 CH CH CH N CH 1-(2-methoxyphenyl)-3- pyrrolidinyl 2755 CH CH CH N CH 1-(3-methoxyphenyl)-3- pyrrolidinyl 2756 CH CH CH N CH 1-(4-methoxyphenyl)-3- pyrrolidinyl 2757 CH CH CH N CH 1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 2758 CH CH CH N CH 1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 2759 CH CH CH N CH 1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 2760 CH CH CH N CH 1-(3,5-difluorophenyl)-3- pyrrolidinyl 2761 CH CH CH N CH 1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 2762 CH CH CH N CH 1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 2763 CH CH CH N CH 1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 2764 CH CH CH N CH 1-(2-pyridyl)-3-pyrrolidinyl 2765 CH CH CH N CH 1-(3-pyridyl)-3-pyrrolidinyl 2766 CH CH CH N CH 1-(4-pyridyl)-3-pyrrolidinyl 2767 CH CH CH N CH 1-(2-pyrirnidinyl)-3-pyrrolidinyl 2768 CH CH CH N CH 5-oxo-1-phenyl-3-pyrrolidinyl 2769 CH CH CH N CH 1-phenyl-3-piperidyl 2770 CH CH CH N CH 1-(2-fluorophenyl)-3-piperidyl 2771 CH CH CH N CH 1-(3-fluorophenyl)-3-piperidyl 2772 CH CH CH N CH 1-(4-fluorophenyl)-3-piperidyl 2773 CH CH CH N CH 1-(2-chlorophenyl)-3-piperidyl 2774 CH CH CH N CH 1-(3-chlorophenyl)-3-piperidyl 2775 CH CH CH N CH 1-(4-chlorophenyl)-3-piperidyl 2776 CH CH CH N CH 1-(2-methylphenyl)-3-piperidyl 2777 CH CH CH N CH 1-(3-methylphenyl)-3-piperidyl 2778 CH CH CH N CH 1-(4-methylphenyl)-3-piperidyl 2779 CH CH CH N CH 1-(2-methoxyphenyl)-3-piperidyl 2780 CH CH CH N CH 1-(3-methoxyphenyl)-3-piperidyl 2781 CH CH CH N CH 1-(4-methoxyphenyl)-3-piperidyl 2782 CH CH CH N CH 1-(2-trifluoromethylphenyl)-3- piperidyl 2783 CH CH CH N CH 1-(3-trifluoromethylphenyl)-3- piperidyl 2784 CH CH CH N CH 1-(4-trifluoromethylphenyl)-3- piperidyl 2785 CH CH CH N CH 1-(3,5-difluorophenyl)-3- piperidyl 2786 CH CH CH N CH 1-(2-difluoromethoxyphenyl)-3- piperidyl 2787 CH CH CH N CH 1-(3-difluoromethoxyphenyl)-3- piperidyl 2788 CH CH CH N CH 1-(4-difluoromethoxyphenyl)-3- piperidyl 2789 CH CH CH N CH 1-(2-pyridyl)-3-piperidyl 2790 CH CH CH N CH 1-(3-pyridyl)-3-piperidyl 2791 CH CH CH N CH 1-(4-pyridyl)-3-piperidyl 2792 CH CH CH N CH 1-phenyl-4-piperidyl 2793 CH CH CH N CH 1-(2-fluorophenyl)-4-piperidyl 2794 CH CH CH N CH 1-(3-fluorophenyl)-4-piperidyl 2795 CH CH CH N CH 1-(4-fluorophenyl)-4-piperidyl 2796 CH CH CH N CH 1-(2-chlorophenyl)-4-piperidyl 2797 CH CH CH N CH 1-(3-chlorophenyl)-4-piperidyl 2798 CH CH CH N CH 1-(4-chlorophenyl)-4-piperidyl 2799 CH CH CH N CH 1-(2-methylphenyl)-4-piperidyl 2800 CH CH CH N CH 1-(3-methylphenyl)-4-piperidyl 2801 CH CH CH N CH 1-(4-methylphenyl)-4-piperidyl 2802 CH CH CH N CH 1-(2-methoxyphenyl)-4-piperidyl 2803 CH CH CH N CH 1-(3-methoxyphenyl)-4-piperidyl 2804 CH CH CH N CH 1-(4-methoxyphenyl)-4-piperidyl 2805 CH CH CH N CH 1-(2-trifluoromethylphenyl)-4- piperidyl 2806 CH CH CH N CH 1-(3-trifluoromethylphenyl)-4- piperidyl 2807 CH CH CH N CH 1-(4-trifluoromethylphenyl)-4- piperidyl 2808 CH CH CH N CH 1-(3,5-difluorophenyl)-4- piperidyl 2809 CH CH CH N CH 1-(2-difluoromethoxyphenyl)-4- piperidyl 2810 CH CH CH N CH 1-(3-difluoromethoxyphenyl)-4- piperidyl 2811 CH CH CH N CH 1-(4-difluoromethoxyphenyl)-4- piperidyl 2812 CH CH CH N CH 1-(2-pyridyl)-4-piperidyl 2813 CH CH CH N CH 1-(3-pyridyl)-4-piperidyl 2814 CH CH CH N CH 1-(4-pyridyl)-4-piperidyl 2815 CH CH CH N CH 3-hydroxymethyl-1-phenyl-4- piperidyl 2816 CH CH CH N CH 3-methoxycarbonyl-1-phenyl-4- piperidyl 2817 CH CH CH N CH 3-ethoxycarbonyl-1-phenyl-4- piperidyl 2818 CH CH CH N CH 3-isopropoxycarbonyl-1-phenyl-4- piperidyl 2819 CH CH CH N CH 4-phenylcyclohexyl 2820 CH CH CH N CH 4-(2-fluorophenyl)cyclohexyl 2821 CH CH CH N CH 4-(3-fluorophenyl)cyclohexyl 2822 CH CH CH N CH 4-(4-fluorophenyl)cyclohexyl 2823 CH CH CH N CH 4-(2-chlorophenyl)cyclohexyl 2824 CH CH CH N CH 4-(3-chlorophenyl)cyclohexyl 2825 CH CH CH N CH 4-(4-chlorophenyl)cyclohexyl 2826 CH CH CH N CH 4-(2-methylphenyl)cyclohexyl 2827 CH CH CH N CH 4-(3-methylphenyl)cyclohexyl 2828 CH CH CH N CH 4-(4-methylphenyl)cyclohexyl 2829 CH CH CH N CH 4-(2-methoxyphenyl)cyclohexyl 2830 CH CH CH N CH 4-(3-methoxyphenyl)cyclohexyl 2831 CH CH CH N CH 4-(4-methoxyphenyl)cyclohexyl 2832 CH CH CH N CH 4-(2-trifluoromethylphenyl)cyclo- hexyl 2833 CH CH CH N CH 4-(3-trifluoromethylphenyl)cyclo- hexyl 2834 CH CH CH N CH 4-(4-trifluoromethylphenyl)cyclo- hexyl 2835 CH CH CH N CH 4-(3,5-difluorophenyl)cyclohexyl 2836 CH CH CH N CH 4-(3-acetylphenyl)cyclohexyl 2837 CH CH CH N CH 4-(3-cyanophenyl)cyclohexyl 2838 CH CH CH N CH 4-(2-difluoromethoxyphenyl)cyclo- hexyl 2839 CH CH CH N CH 4-(3-difluoromethoxyphenyl)cyclo- hexyl 2840 CH CH CH N CH 4-(4-difluoromethoxyphenyl)cyclo- hexyl 2841 CH CH CH N CH 4-(2-pyridyl)cyclohexyl 2842 CH CH CH N CH 4-(3-pyridyl)cyclohexyl 2843 CH CH CH N CH 4-(4-pyridyl)cyclohexyl 2844 CH CH CH N CH 4-(4-fluoro-3-pyridyl)cyclohexyl 2845 CH CH CH N CH 4-(3-quinolyl)cyclohexyl 2846 CH CH CH N CH 4-(3-fluorophenyl)-4-hydroxy- cyclohexyl 2847 CH CH CH N CH 3-phenylcyclohexyl 2848 CH CH CH N CH 3-phenylcyclopentyl 2849 CH CH CH N CH 6-phenyl-3-tetrahydropyranyl 2850 CH CH CH N CH 6-(3-fluorophenyl)-3-tetrahydro- pyranyl 2851 CH CH CH N CH 2-phenylcyclopropyl 2852 CH CH CH N CH 2-(2-pyridyl)cyclopropyl 2853 CH CH CH N CH 2-(3-pyridyl)cyclopropyl 2854 CH CH CH N CH 2-(4-pyridyl)cyclopropyl 2855 CH CH CH N CH 2-(3-fluorophenyl)cyclopropyl 2856 CH CH CH N CH 2-indanyl 2857 CH CH CH N CH 2-tetrahydronaphthyl 2858 CH CH CH N CH 6-methoxy-2-tetrahydronaphthyl 2859 CH CH CH N CH benzyl 2860 CH CH CH N CH phenethyl 2861 CH CH CH N CH 3-phenylpropyl 2862 CH CH CH N CH 4-phenylbutyl 2863 CH CH CH N CH 2-methoxyphenethyl 2864 CH CH CH N CH 3-methoxyphenethyl 2865 CH CH CH N CH 4-methoxyphenethyl 2866 CH CH CH N CH 4-fluorophenethyl 2867 CH CH CH N CH 4-bromophenethyl 2868 CH CH CH N CH 4-chlorophenethyl 2869 CH CH CH N CH 3-trifluoromethylphenethyl 2870 CH CH CH N CH 3,4-dimethoxyphenethyl 2871 CH CH CH N CH 3-propoxyphenethyl 2872 CH CH CH N CH 3,5-difluorophenethyl 2873 CH CH CH N CH 4-dimethylaminophenethyl 2874 CH CH CH N CH 3-difluoromethoxyphenethyl 2875 CH CH CH N CH 2-methylphenethyl 2876 CH CH CH N CH 4-acetylphenethyl 2877 CH CH CH N CH 4-dimethylamino-2-methoxy- phenethyl 2878 CH CH CH N CH cyclohexylethyl 2879 CH CH CH N CH 2-(2-pyridyl)ethyl 2880 CH CH CH N CH 2-(3-pyridyl)ethyl 2881 CH CH CH N CH 2-(4-pyridyl)ethyl 2882 CH CH CH N CH 2-(2-quinolyl)ethyl 2883 CH CH CH N CH 2-(3-quinolyl)ethyl 2884 CH CH CH N CH 2-(4-quinolyl)ethyl 2885 CH CH CH N CH 2-(6-quinolyl)ethyl 2886 CH CH CH N CH 2-(2-indolyl)ethyl 2887 CH CH CH N CH 2-(3-indolyl)ethyl 2888 CH CH CH N CH 2-(7-aza-3-indolyl)ethyl 2889 CH CH CH N CH 2-(benzimidazolyl)ethyl 2890 CH CH CH N CH 2-(benzoxazolyl)ethyl 2891 CH CH CH N CH 2-(benzothiazolyl)ethyl 2892 CH CH CH N CH 2-(1-naphthyl)ethyl 2893 CH CH CH N CH 2-(2-naphthyl)ethyl 2894 CH CH CH N CH 1-(hydroxymethyl)-2-phenylethyl 2895 CH CH CH N CH 1-(methoxycarbonyl)-2-phenylethyl 2896 CH CH CH N CH 1-(ethoxycarbonyl)-2-phenylethyl 2897 CH CH CH N CH 1-carboxy-2-phenylethyl 2898 CH CH CH N CH 1-(benzyloxycarbonyl)-2- phenylethyl 2899 CH CH CH N CH 1-(phenoxymethyl)-2-phenylethyl 2900 CH CH CH N CH 1-(benzyloxymethyl)-2-phenyl- ethyl 2901 CH CH CH N CH 1-(benzylcarbamoyl)-2-phenylethyl 2902 CH CH CH N CH 1-(N-methylbenzylcarbanioyl)-2- phenylethyl 2903 CH CH CH N CH 1-(phenylcarbamoyl)-2-phenyl- ethyl 2904 CH CH CH N CH 1-(N-methylphenylcarbamoyl)-2- phenylethyl 2905 CH CH CH N CH 1-(N-benzylaminomethyl)-2- phenylethyl 2906 CH CH CH N CH 1-(N-benzyl-N-methylamino- methyl)-2-phenylethyl 2907 CH CH CH N CH 1-(anilinomethyl)-2-phenylethyl 2908 CH CH CH N CH 1-(N-methylanilinomethyl)-2- phenylethyl 2909 CH CH CH N CH 1-(N-methylaminomethyl)-2-phenyl- ethyl 2910 CH CH CH N CH 1-(N-ethylaminomethyl)-2-phenyl- ethyl 2911 CH CH CH N CH 1-(N-isobutylaminomethyl)-2- phenylethyl 2912 CH CH CH N CH 1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 2913 CH CH CH N CH 1-(aminomethyl)-2-phenylethyl 2914 CH CH CH N CH 1-benzyl-2-(2-pyridylmethyl- amino)ethyl 2915 CH CH CH N CH 1-benzyl-2-(3-pyridylmethyl- amino)ethyl 2916 CH CH CH N CH 1-benzyl-2-(4-pyridylmethyl- amino)ethyl 2917 CH CH CH N CH 2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 2918 CH CH CH N CH 2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 2919 CH CH CH N CH 2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 2920 CH CH CH N CH 2-hydroxy-2-phenylethyl 2921 CH CH CH N CH benzoylmethyl 2922 CH CH CH N CH 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 2923 CH CH CH N CH 1-(benzyloxycarbonyl)-2-cyclo- hexylethyl 2924 CH CH CH N CH 1-(phenoxymethyl)-2-(3- indolyl)ethyl 2925 CH CH CH N CH 2-(2-methoxyphenoxy)ethyl 2926 CH CH CH N CH 1-(benzylcarbamoyl)-2-cyclo- hexylethyl 2927 CH CH CH N CH 1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 2928 CH CH CH N CH 1-(phenylcarbamoyl)-2- cyclohexylethyl 2929 CH CH CH N CH 1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 2930 CH CH CH N CH 1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 2931 CH CH CH N CH 1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 2932 CH CH CH N CH 1-(benzylcarbamoyl)-2-(4- pyridyl)ethyl 2933 CH CH CH N CH 1-(4-pyridylmethylcarbamoyl)-2-(4- fluorophenyl)ethyl 2934 CH CH CH N CH 1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 2935 CH CH CH N CH 1-(benzyloxymethyl)-2-(2- indolyl)ethyl 2936 CH CH CH N CH 1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 2937 CH CH CH N CH 1-(N-methylbenzylcarbamoyl)-2- (3-pyridyl)ethyl 2938 CH CH CH N CH 2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 2939 CH CH CH N CH 2-hydroxy-2-(2-quinolyl)ethyl 2940 CH CH CH N CH 2-hydroxy-2-(3-quinolyl)ethyl 2941 CH CH CH N CH 2-hydroxy-2-(4-quinolyl)ethyl 2942 CH CH CH N CH 2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 2943 CH CH CH N CH 1-carboxy-2-cyclohexylethyl 2944 CH CH CH N CH 2-hydroxy-2-(6-quinolyl)ethyl 2945 CH CH CH N CH 2-(benzylamino)-2-phenylethyl 2946 CH CH CH N CH 2-amino-2-(2-naphthyl)propyl 2947 CH CH CH N CH 2-(phenylamino)ethyl 2948 CH CH CH N CH diphenylmethyl 2949 CH CH CH N CH 2,2-diphenylethyl 2950 CH CH CH N CH 2-phenyl-2-(2-pyridyl)ethyl 2951 CH CH CH N CH 2-phenyl-2-(3-pyridyl)ethyl 2952 CH CH CH N CH 2-phenyl-2-(4-pyridyl)ethyl 2953 CH CH CH N CH 2-phenoxy-2-phenylethyl 2954 CH CH CH N CH 2-(benzyloxy)-2-phenylethyl 2955 CH CH CH N N 1-phenyl-3-pyrrolidinyl 2956 CH CH CH N N 1-(2-fluorophenyl)-3-pyrrolidinyl 2957 CH CH CH N N 1-(3-fluorophenyl)-3-pyrrolidinyl 2958 CH CH CH N N 1-(4-fluorophenyl)-3-pyrrolidinyl 2959 CH CH CH N N 1-(2-chlorophenyl)-3-pyrrolidinyl 2960 CH CH CH N N 1-(3-chlorophenyl)-3-pyrrolidinyl 2961 CH CH CH N N 1-(4-chlorophenyl)-3-pyrrolidinyl 2962 CH CH CH N N 1-(2-methylphenyl)-3-pyrrolidinyl 2963 CH CH CH N N 1-(3-methylphenyl)-3-pyrrolidinyl 2964 CH CH CH N N 1-(4-methylphenyl)-3-pyrrolidinyl 2965 CH CH CH N N 1-(2-methoxyphenyl)-3-pyrrolidinyl 2966 CH CH CH N N 1-(3-methoxyphenyl)-3-pyrrolidinyl 2967 CH CH CH N N 1-(4-methoxyphenyl)-3-pyrrolidinyl 2968 CH CH CH N N 1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 2969 CH CH CH N N 1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 2970 CH CH CH N N 1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 2971 CH CH CH N N 1-(3,5-difluorophenyl)-3- pyrrolidinyl 2972 CH CH CH N N 1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 2973 CH CH CH N N 1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 2974 CH CH CH N N 1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 2975 CH CH CH N N 1-(2-pyridyl)-3-pyrrolidinyl 2976 CH CH CH N N 1-(3-pyridyl)-3-pyrrolidinyl 2977 CH CH CH N N 1-(4-pyridyl)-3-pyrrolidinyl 2978 CH CH CH N N 1-(2-pyrimidinyl)-3-pyrrolidinyl 2979 CH CH CH N N 5-oxo-1-phenyl-3-pyrrolidinyl 2980 CH CH CH N N 1-phenyl-3-piperidyl 2981 CH CH CH N N 1-(2-fluorophenyl)-3-piperidyl 2982 CH CH CH N N 1-(3-fluorophenyl)-3-piperidyl 2983 CH CH CH N N 1-(4-fluorophenyl)-3-piperidyl 2984 CH CH CH N N 1-(2-chlorophenyl)-3-piperidyl 2985 CH CH CH N N 1-(3-chlorophenyl)-3-piperidyl 2986 CH CH CH N N 1-(4-chlorophenyl)-3-piperidyl 2987 CH CH CH N N 1-(2-methylphenyl)-3-piperidyl 2988 CH CH CH N N 1-(3-methylphenyl)-3-piperidyl 2989 CH CH CH N N 1-(4-methylphenyl)-3-piperidyl 2990 CH CH CH N N 1-(2-methoxyphenyl)-3-piperidyl 2991 CH CH CH N N 1-(3-methoxyphenyl)-3-piperidyl 2992 CH CH CH N N 1-(4-methoxyphenyl)-3-piperidyl 2993 CH CH CH N N 1-(2-trifuoromethylphenyl)-3- piperidyl 2994 CH CH CH N N 1-(3-trifuoromethylphenyl)-3- piperidyl 2995 CH CH CH N N 1-(4-trifuoromethylphenyl)-3- piperidyl 2996 CH CH CH N N 1-(3,5-difluorophenyl)-3- piperidyl 2997 CH CH CH N N 1-(2-difluoromethoxyphenyl)-3- piperidyl 2998 CH CH CH N N 1-(3-difluoromethoxyphenyl)-3- piperidyl 2999 CH CH CH N N 1-(4-difluoromethoxyphenyl)-3- piperidiyl 3000 CH CH CH N N 1-(2-pyridyl)-3-piperidyl 3001 CH CH CH N N 1-(3-pyridyl)-3-piperidyl 3002 CH CH CH N N 1-(4-pyridyl)-3-piperidyl 3003 CH CH CH N N 1-phenyl-4-piperidyl 3004 CH CH CH N N 1-(2-fluorophenyl)-4-piperidyl 3005 CH CH CH N N 1-(3-fluorophenyl)-4-piperidyl 3006 CH CH CH N N 1-(4-fluorophenyl)-4-piperidyl 3007 CH CH CH N N 1-(2-chlorophenyl)-4-piperidyl 3008 CH CH CH N N 1-(3-chlorophenyl)-4-piperidyl 3009 CH CH CH N N 1-(4-chlorophenyl)-4-piperidyl 3010 CH CH CH N N 1-(2-methylphenyl)-4-piperidyl 3011 CH CH CH N N 1-(3-methylphenyl)-4-piperidyl 3012 CH CH CH N N 1-(4-methylphenyl)-4-piperidyl 3013 CH CH CH N N 1-(2-methoxyphenyl)-4-piperidyl 3014 CH CH CH N N 1-(3-methoxyphenyl)-4-piperidyl 3015 CH CH CH N N 1-(4-methoxyphenyl)-4-piperidyl 3016 CH CH CH N N 1-(2-trifluoromethylphenyl)-4- piperidyl 3017 CH CH CH N N 1-(3-trifluoromethylphenyl)-4- piperidyl 3018 CH CH CH N N 1-(4-trifluoromethylphenyl)-4- piperidyl 3019 CH CH CH N N 1-(3,5-difluorophenyl)-4- piperidyl 3020 CH CH CH N N 1-(2-difluoromethoxyphenyl)-4- piperidyl 3021 CH CH CH N N 1-(3-difluoromethoxyphenyl)-4- piperidyl 3022 CH CH CH N N 1-(4-difluoromethoxyphenyl)-4- piperidyl 3023 CH CH CH N N 1-(2-pyridyl)-4-piperidyl 3024 CH CH CH N N 1-(3-pyridyl)-4-piperidyl 3025 CH CH CH N N 1-(4-pyridyl)-4-piperidyl 3026 CH CH CH N N 3-hydroxymethyl-1-phenyl-4- piperidyl 3027 CH CH CH N N 3-methoxycarbonyl-1-phenyl-4- piperidyl 3028 CH CH CH N N 3-ethoxycarbonyl-1-phenyl-4- piperidyl 3029 CH CH CH N N 3-isopropoxycarbonyl-1-phenyl-4- piperidyl 3030 CH CH CH N N 4-phenylcyclohexyl 3031 CH CH CH N N 4-(2-fluorophenyl)cyclohexyl 3032 CH CH CH N N 4-(3-fluorophenyl)cyclohexyl 3033 CH CH CH N N 4-(4-fluorophenyl)cyclohexyl 3034 CH CH CH N N 4-(2-chlorophenyl)cyclohexyl 3035 CH CH CH N N 4-(3-chlorophenyl)cyclohexyl 3036 CH CH CH N N 4-(4-chlorophenyl)cyclohexyl 3037 CH CH CH N N 4-(2-methylphenyl)cyclohexyl 3038 CH CH CH N N 4-(3-methylphenyl)cyclohexyl 3039 CH CH CH N N 4-(4-methylphenyl)cyclohexyl 3040 CH CH CH N N 4-(2-methoxyphenyl)cyclohexyl 3041 CH CH CH N N 4-(3-methoxyphenyl)cyclohexyl 3042 CH CH CH N N 4-(4-methoxyphenyl)cyclohexyl 3043 CH CH CH N N 4-(2-trifluoromethylphenyl)cyclo- hexyl 3044 CH CH CH N N 4-(3-trifluoromethylphenyl)cyclo- hexyl 3045 CH CH CH N N 4-(4-trifluoromethylphenyl)cyclo- hexyl 3046 CH CH CH N N 4-(3,5-difluorophenyl)cyclohexyl 3047 CH CH CH N N 4-(3-acetylphenyl)cyclohexyl 3048 CH CH CH N N 4-(3-cyanophenyl)cyclohexyl 3049 CH CH CH N N 4-(2-difluoromethoxyphenyl)cyclo- hexyl 3050 CH CH CH N N 4-(3-difluoromethoxyphenyl)cyclo- hexyl 3051 CH CH CH N N 4-(4-difluoromethoxyphenyl)cyclo- hexyl 3052 CH CH CH N N 4-(2-pyridyl)cyclohexyl 3053 CH CH CH N N 4-(3-pyridyl)cyclohexyl 3054 CH CH CH N N 4-(4-pyridyl)cyclohexyl 3055 CH CH CH N N 4-(4-fluoro-3-pyridyl)cyclohexyl 3056 CH CH CH N N 4-(3-quinolyl)cyclohexyl 3057 CH CH CH N N 4-(3-fluorophenyl)-4-hydroxy- cyclohexyl 3058 CH CH CH N N 3-phenylcyclohexyl 3059 CH CH CH N N 3-phenylcyclopentyl 3060 CH CH CH N N 6-phenyl-3-tetrahydropyranyl 3061 CH CH CH N N 6-(3-fluorophenyl)-3-tetrahydro- pyranyl 3062 CH CH CH N N 2-phenylcyclopropyl 3063 CH CH CH N N 2-(2-pyridyl)cyclopropyl 3064 CH CH CH N N 2-(3-pyridyl)cyclopropyl 3065 CH CH CH N N 2-(4-pyridyl)cyclopropyl 3066 CH CH CH N N 2-(3-fluorophenyl)cyclopropyl 3067 CH CH CH N N 2-indanyl 3068 CH CH CH N N 2-tetrahydronaphthyl 3069 CH CH CH N N 6-methoxy-2-tetrahydronaphthyl 3070 CH CH CH N N benzyl 3071 CH CH CH N N phenethyl 3072 CH CH CH N N 3-phenylpropyl 3073 CH CH CH N N 4-phenylbutyl 3074 CH CH CH N N 2-methoxyphenethyl 3075 CH CH CH N N 3-methoxyphenethyl 3076 CH CH CH N N 4-methoxyphenethyl 3077 CH CH CH N N 4-fluorophenethyl 3078 CH CH CH N N 4-bromophenethyl 3079 CH CH CH N N 4-chlorophenethyZL 3080 CH CH CH N N 3-trifluoromethylphenethyl 3081 CH CH CH N N 3,4-dimethoxyphenethyl 3082 CH CH CH N N 3-propoxyphenethyl 3083 CH CH CH N N 3,5-difluorophenethyl 3084 CH CH CH N N 4-dimethylaminophenethyl 3085 CH CH CH N N 3-difluoromethoxyphenethyl 3086 CH CH CH N N 2-methylphenethyl 3087 CH CH CH N N 4-acetylphenethyl 3088 CH CH CH N N 4-dimethylamino-2-methoxyphenethyl 3089 CH CH CH N N cyclohexylethyl 3090 CH CH CH N N 2-(2-pyridyl)ethyl 3091 CH CH CH N N 2-(3-pyridyl)ethyl 3092 CH CH CH N N 2-(4-pyridyl)ethyl 3093 CH CH CH N N 2-(2-quinolyl)ethyl 3094 CH CH CH N N 2-(3-quinolyl)ethyl 3095 CH CH CH N N 2-(4-quinolyl)ethyl 3096 CH CH CH N N 2-(6-quinolyl)ethyl 3097 CH CH CH N N 2-(2-indolyl)ethyl 3098 CH CH CH N N 2-(3-indolyl)ethyl 3099 CH CH CH N N 2-(7-aza-3-indolyl)ethyl 3100 CH CH CH N N 2-(benzimidazolyl)ethyl 3101 CH CH CH N N 2-(benzoxazolyl)ethyl 3102 CH CH CH N N 2-(benzothiazolyl)ethyl 3103 CH CH CH N N 2-(1-naphthyl)ethyl 3104 CH CH CH N N 2-(2-naphthyl)ethyl 3105 CH CH CH N N 1-(hydroxymethyl)-2-phenylethyl 3106 CH CH CH N N 1-(methoxycarbonyl)-2-phenylethyl 3107 CH CH CH N N 1-(ethoxycarbonyl)-2-phenylethyl 3108 CH CH CH N N 1-carboxy-2-phenylethyl 3109 CH CH CH N N 1-(benzyloxycarbonyl)-2-phenyl- ethyl 3110 CH CH CH N N 1-(phenoxymethyl)-2-phenylethyl 3111 CH CH CH N N 1-(benzyloxymethyl)-2-phenylethyl 3112 CH CH CH N N 1-(benzylcarbamoyl)-2-phenylethyl 3113 CH CH CH N N 1-(N-methylbenzylcarbamoyl)-2- phenylethyl 3114 CH CH CH N N 1-(phenylcarbamoyl)-2-phenylethyl 3115 CH CH CH N N 1-(N-methylphenylcarbamoyl)-2- phenylethyl 3116 CH CH CH N N 1-(N-benzylaminomethyl)-2- phenylethyl 3117 CH CH CH N N 1-(N-benzyl-N-methylaminomethyl)- 2-phenylethyl 3118 CH CH CH N N 1-(anilinomethyl)-2-phenylethyl 3119 CH CH CH N N 1-(N-methylanilinomethyl)-2- phenylethyl 3120 CH CH CH N N 1-(N-methylaminomethyl)-2- phenylethyl 3121 CH CH CH N N 1-(N-ethylaminomethyl)-2- phenylethyl 3122 CH CH CH N N 1-(N-isobutylaminomethyl)-2- phenylethyl 3123 CH CH CH N N 1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 3124 CH CH CH N N 1-(aminomethyl)-2-phenylethyl 3125 CH CH CH N N 1-benzyl-2-(2-pyridylmethyl- amino)ethyl 3126 CH CH CH N N 1-benzyl-2-(3-pyridylmethyl- amino)ethyl 3127 CH CH CH N N 1-benzyl-2-(4-pyridylmethyl- amino)ethyl 3128 CH CH CH N N 2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 3129 CH CH CH N N 2-phenyl-1-(3-pyridylmethyl- carbanioyl)ethyl 3130 CH CH CH N N 2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 3131 CH CH CH N N 2-hydroxy-2-phenylethyl 3132 CH CH CH N N benzoylmethyl 3133 CH CH CH N N 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 3134 CH CH CH N N 1-(benzyloxycarbonyl)-2- cyclohexylethyl 3135 CH CH CH N N 1-(phenoxymethyl)-2-(3- indolyl)ethyl 3136 CH CH CH N N 2-(2-methoxyphenoxy)ethyl 3137 CH CH CH N N 1-(benzylcarbamoyl)-2- cyclohexylethyl 3138 CH CH CH N N 1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 3139 CH CH CH N N 1-(phenylcarbamoyl)-2- cyclohexylethyl 3140 CH CH CH N N 1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 3141 CH CH CH N N 1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 3142 CH CH CH N N 1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 3143 CH CH CH N N 1-(benzylcarbarnoyl)-2-(4- pyridyl)ethyl 3144 CH CH CH N N 1-(4-pyridylmethylcarbamoyl)-2-(4- fluorophenyl)ethyl 3145 CH CH CH N N 1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 3146 CH CH CH N N 1-(benzyloxymethyl)-2-(2- indolyl)ethyl 3147 CH CH CH N N 1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 3148 CH CH CH N N 1-(N-methylbenzylcarbamoyl)-2-(3- pyridyl)ethyl 3149 CH CH CH N N 2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 3150 CH CH CH N N 2-hydroxy-2-(2-quinolyl)ethyl 3151 CH CH CH N N 2-hydroxy-2-(3-quinolyl)ethyl 3152 CH CH CH N N 2-hydroxy-2-(4-quinolyl)ethyl 3153 CH CH CH N N 3-hydroxy-2-(3,5-difluoro- phenyl)ethyl 3154 CH CH CH N N 1-carboxy-2-cyclohexylethyl 3155 CH CH CH N N 2-hydroxy-2-(6-quinolyl)ethyl 3156 CH CH CH N N 2-(benzylamino)-2-phenylethyl 3157 CH CH CH N N 2-amino-2-(2-naphthyl)propyl 3158 CH CH CH N N 2-(phenylamino)ethyl 3159 CH CH CH N N diphenylmethyl 3160 CH CH CH N N 2,2-diphenylethyl 3161 CH CH CH N N 2-phenyl-2-(2-pyridyl)ethyl 3162 CH CH CH N N 2-phenyl-2-(3-pyridyl)ethyl 3163 CH CH CH N N 2-phenyl-2-(4-pyridyl)ethyl 3164 CH CH CH N N 2-phenoxy-2-phenylethyl 3165 CH CH CH N N 2-(benzyloxy)-2-phenylethyl

[0157] TABLE 4

No. A—Ar¹—R⁰ 3157′ 1-phenyl-3-pyrrolidinyl 3158′ 1-(2-fluorophenyl)-3-pyrrolidinyl 3159′ 1-(3-fluorophenyl)-3-pyrrolidinyl 3160′ 1-(4-fluorophenyl)-3-pyrrolidinyl 3161′ 1-(2-chlorophenyl)-3-pyrrolidinyl 3162′ 1-(3-chlorophenyl)-3-pyrrolidinyl 3163′ 1-(4-chlorophenyl)-3-pyrrolidinyl 3164′ 1-(2-methylphenyl)-3-pyrrolidinyl 3165′ 1-(3-methyiphenyl)-3-pyrrolidinyl 3166 1-(4-methylphenyl)-3-pyrrolidinyl 3167 1-(2-methoxyphenyl)-3-pyrrolidinyl 3168 1-(3-methoxyphenyl)-3-pyrrolidinyl 3169 1-(4-methoxyphenyl)-3-pyrrolidinyl 3170 1-(2-trifluoromethylphenyl)-3-pyrrolidinyl 3171 1-(3-trifluoromethylphenyl)-3-pyrrolidinyl 3172 1-(4-trifluoromethylphenyl)-3-pyrrolidinyl 3173 1-(3,5-difluorophenyl)-3-pyrrolidinyl 3174 1-(2-difluoromethoxyphenyl)-3-pyrrolidinyl 3175 1-(3-difluoromethoxyphenyl)-3-pyrrolidinyl 3176 1-(4-difluoromethoxyphenyl)-3-pyrrolidinyl 3177 1-(2-pyridyl)-3-pyrrolidinyl 3178 1-(3-pyridyl)-3-pyrrolidinyl 3179 1-(4-pyridyl)-3-pyrrolidinyl 3180 1-(2-pyrimidinyl)-3-pyrrolidinyl 3181 5-oxo-1-phenyl-3-pyrrolidinyl 3182 1-phenyl-3-piperidyl 3183 1-(2-fluorophenyl)-3-piperidyl 3184 1-(3-fluorophenyl)-3-piperidyl 3185 1-(4-fluorophenyl)-3-piperidyl 3186 1-(2-chlorophenyl)-3-piperidyl 3187 1-(3-chlorophenyl)-3-piperidyl 3188 1-(4-chlorophenyl)-3-piperidyl 3189 1-(2-methylphenyl)-3-piperidyl 3190 1-(3-methylphenyl)-3-piperidyl 3191 1-(4-methylphenyl)-3-piperidyl 3192 1-(2-methoxyphenyl)-3-piperidyl 3193 1-(3-methoxyphenyl)-3-piperidyl 3194 1-(4-methoxyphenyl)-3-piperidyl 3195 1-(2-trifluoromethylphenyl)-3-piperidyl 3196 1-(3-trifluoromethylphenyl)-3-piperidyl 3197 1-(4-trifluoromethylphenyl)-3-piperidyl 3198 1-(3,5-difluorophenyl)-3-piperidyl 3199 1-(2-difluoromethoxyphenyl)-3-piperidyl 3200 1-(3-difluoromethoxyphenyl)-3-piperidyl 3201 1-(4-difluoromethoxyphenyl)-3-piperidyl 3202 1-(2-pyridyl)-3-piperidyl 3203 1-(3-pyridyl)-3-piperidyl 3204 1-(4-pyridyl)-3-piperidyl 3205 1-phenyl-4-piperidyl 3206 1-(2-fluorophenyl)-4-piperidyl 3207 1-(3-fluorophenyl)-4-piperidyl 3208 1-(4-fluorophenyl)-4-piperidyl 3209 1-(2-chlorophenyl)-4-piperidyl 3210 1-(3-chlorophenyl)-4-piperidyl 3211 1-(4-chlorophenyl)-4-piperidyl 3212 1-(2-methylphenyl)-4-piperidyl 3213 1-(3-methylphenyl)-4-piperidyl 3214 1-(4-methylphenyl)-4-piperidyl 3215 1-(2-methoxyphenyl)-4-piperidyl 3216 1-(3-methoxyphenyl)-4-piperidyl 3217 1-(4-methoxyphenyl)-4-piperidyl 3218 1-(2-trifluoromethylphenyl)-4-piperidyl 3219 1-(3-trifluoromethylphenyl)-4-piperidyl 3220 1-(4-trifluoromethylphenyl)-4-piperidyl 3221 1-(3,5-difluorophenyl)-4-piperidyl 3222 1-(2-difluoromethoxyphenyl)-4-piperidyl 3223 1-(3-difluoromethoxyphenyl)-4-piperidyl 3224 1-(4-difluoromethoxyphenyl)-4-piperidyl 3225 1-(2-pyridyl)-4-piperidyl 3226 1-(3-pyridyl)-4-piperidyl 3227 1-(4-pyridyl)-4-piperidyl 3228 3-hydroxymethyl-1-phenyl-4-piperidyl 3229 3-methoxycarbonyl-1-phenyl-4-piperidyl 3230 3-ethoxycarbonyl-1-phenyl-4-piperidyl 3231 3-isopropoxycarbonyl-1-phenyl-4-piperidyl 3232 4-phenylcyclohexyl 3233 4-(2-fluorophenyl)cyclohexyl 3234 4-(3-fluorophenyl)cyclohexyl 3235 4-(4-fluorophenyl)cyclohexyl 3236 4-(2-chlorophenyl)cyclohexyl 3237 4-(3-chlorophenyl)cyclohexyl 3238 4-(4-chlorophenyl)cyclohexyl 3239 4-(2-methylphenyl)cyclohexyl 3240 4-(3-methylphenyl)cyclohexyl 3241 4-(4-methylphenyl)cyclohexyl 3242 4-(2-methoxyphenyl)cyclohexyl 3243 4-(3-methoxyphenyl)cyclohexyl 3244 4-(4-methoxyphenyl)cyclohexyl 3245 4-(2-trifluoromethylphenyl)cyclohexyl 3246 4-(3-trifluoromethylphenyl)cyclohexyl 3247 4-(4-trifluoromethylphenyl)cyclohexyl 3248 4-(3,5-difluorophenyl)cyclohexyl 3249 4-(3-acetylphenyl)cyclohexyl 3250 4-(3-cyanophenyl)cyclohexyl 3251 4-(2-difluoromethoxyphenyl)cyclohexyl 3252 4-(3-difluoromethoxyphenyl)cyclohexyl 3253 4-(4-difluoromethoxyphenyl)cyclohexyl 3254 4-(2-pyridyl)cyclohexyl 3255 4-(3-pyridyl)cyclohexyl 3256 4-(4-pyridyl)cyclohexyl 3257 4-(4-fluoro-3-pyridyl)cyclohexyl 3258 4-(3-quinolyl)cyclohexyl 3259 4-(3-fluorophenyl)-4-hydroxycyclohexyl 3260 3-phenylcyclohexyl 3261 3-phenylcyclopentyl 3262 6-phenyl-3-tetrahydropyranyl 3263 6-(3-fluorophenyl)-3-tetrahydropyranyl 3264 2-phenylcyclopropyl 3265 2-(2-pyridyl)cyclopropyl 3266 2-(3-pyridyl)cyclopropyl 3267 2-(4-pyridyl)cyclopropyl 3268 2-(3-fluorophenyl)cyclopropyl 3269 2-indanyl 3270 2-tetrahydronaphthyl 3271 6-methoxy-2-tetrahydronaphthyl 3272 benzyl 3273 phenethyl 3274 3-phenylpropyl 3275 4-phenylbutyl 3276 2-methoxyphenethyl 3277 3-methoxyphenethyl 3278 4-methoxyphenethyl 3279 4-fluorophenethyl 3280 4-bromophenethyl 3281 4-chlorophenethyl 3282 3-trifluoromethylphenethyl 3283 3,4-dimethoxyphenethyl 3284 3-propoxyphenethyl 3285 3,5-difluorophenethyl 3286 4-dimethylaminophenethyl 3287 3-difluoromethoxyphenethyl 3288 2-methylphenethyl 3289 4-acetylphenethyl 3290 4-dimethylamino-2-methoxyphenethyl 3291 cyclohexylethyl 3292 2-(2-pyridyl)ethyl 3293 2-(3-pyridyl)ethyl 3294 2-(4-pyridyl)ethyl 3295 2-(2-quinolyl)ethyl 3296 2-(3-quinolyl)ethyl 3297 2-(4-quinolyl)ethyl 3298 2-(6-quinolyl)ethyl 3299 2-(2-indolyl)ethyl 3300 2-(3-indolyl)ethyl 3301 2-(7-aza-3-indolyl)ethyl 3302 2-(benzimidazolyl)ethyl 3303 2-(benzoxazolyl)ethyl 3304 2-(benzothiazolyl)ethyl 3305 2-(1-naphthyl)ethyl 3306 2-(2-naphthyl)ethyl 3307 1-(hydroxyrnethyl)-2-phenylethyl 3308 1-(methoxycarbonyl)-2-phenylethyl 3309 1-(ethoxycarbonyl)-2-phenylethyl 3310 1-carboxy-2-phenylethyl 3311 1-(benzyloxycarbonyl)-2-phenylethyl 3312 1-(phenoxymethyl)-2-phenylethyl 3313 1-(benzyloxymethyl)-2-phenylethyl 3314 1-(benzylcarbamoyl)-2-phenylethyl 3315 1-(N-methylbenzylcarbamoyl)-2-phenylethyl 3316 1-(phenylcarbamoyl)-2-phenylethyl 3317 1-(N-methylphenylcarbanioyl)-2-phenylethyl 3318 1-(N-benzylaminomethyl)-2-phenylethyl 3319 1-(N-benzyl-N-methylaminomethyl)-2-phenylethyl 3320 1-(anilinomethyl)-2-phenylethyl 3321 1-(N-methylanilinomethyl)-2-phenylethyl 3322 1-(N-methylaniinomethyl)-2-phenylethyl 3323 1-(N-ethylaminomethyl)-2-phenylethyl 3324 1-(N-isobutylaminomethyl)-2-phenylethyl 3325 1-(N-cyclopropylmethylaminomethyl)-2-phenylethyl 3326 1-(aminomethyl)-2-phenylethyl 3327 1-benzyl-2-(2-pyridylmethylamino)ethyl 3328 1-benzyl-2-(3-pyridylmethylamino)ethyl 3329 1-benzyl-2-(4-pyridylmethylaniino)ethyl 3330 2-phenyl-1-(2-pyridylmethylcarbamoyl)ethyl 3331 2-phenyl-1-(3-pyridylmethylcarbamoyl)ethyl 3332 2-phenyl-1-(4-pyridylmethylcarbamoyl)ethyl 3333 2-hydroxy-2-phenylethyl 3334 benzoylmethyl 3335 1-(benzyloxycarbonyl)-2-(3-indolyl)ethyl 3336 1-(benzyloxycarbonyl)-2-cyclohexylethyl 3337 1-(phenoxymethyl)-2-(3-indolyl)ethyl 3338 2-(2-methoxyphenoxyy)ethyl 3339 1-(benzylcarbarnoyl)-2-cyclohexylethyl 3340 1-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 3341 1-(phenylcarbamoyl)-2-cyclohexylethyl 3342 1-(N-methylphenylcarbamoyl)-2-cyclohexylethyl 3343 1-(benzyloxycarbonyl)-2-(3-pyridyl)ethyl 3344 1-(benzylaminomethyl)-2-(3-pyridyl)ethyl 3345 1-(benzylcarbamoyl)-2-(4-pyridyl)ethyl 3346 1-(4-pyridylmethylcarbamoyl)-2-(4-fluorophenyl)ethyl 3347 1-(benzylcarbamoyl)-2-(7-aza-3-indolyl)ethyl 3348 1-(benzyloxymethyl)-2-(2-indolyl)ethyl 3349 1-(N-benzyl-N-methylaminomethyl)-2-(3-pyridyl)ethyl 3350 1-(N-methylbenzylcarbamoyl)-2-(3-pyridyl)ethyl 3351 2-hydroxy-2-(4-dimethylaminophenyl)ethyl 3352 2-hydroxy-2-(2-quinolyl)ethyl 3353 2-hydroxy-2-(3-quinolyl)ethyl 3354 2-hydroxy-2-(4-quinolyl)ethyl 3355 2-hydroxy-2-(3,5-difluorophenyl)ethyl 3356 1-carboxy-2-cyclohexylethyl 3357 2-hydroxy-2-(6-quinolyl)ethyl 3358 2-(benzylamino)-2-phenylethyl 3359 2-amino-2-(2-naphthyl)propyl 3360 2-(phenylamino)ethyl 3361 diphenylmethyl 3362 2,2-diphenylethyl 3363 2-phenyl-2-(2-pyridyl)ethyl 3364 2-phenyl-2-(3-pyridyl)ethyl 3365 2-phenyl-2-(4-pyridyl)ethyl 3366 2-phenoxy-2-phenylethyl 3367 2-(benzyloxy)-2-phenylethyl

[0158] Among the above compounds, the preferred examples are trans-3′-oxo-N-(trans-4-phenylcyclohexyl)spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[(3S)-1-(2-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[(3S)-1-(3-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[(3S)-1-(4-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[1-(2-fluorophenyl)-4-piperidyl]-3′-oxospiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3′-oxospiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[1-(4-fluorophenyl)-4-piperidyl]-3′-oxospiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-3′-oxo-N-(1,2,3,4-tetrahydro-2-naphthyl)spiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[4-azaisobenzofuran-1(3H), 1′-cyclohexane]-4′-carboxamide, trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H), 1′-cyclohexane]-4′-carboxamide, trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[7-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-(6-methoxy-1,2,3,4-tetrahydro-2-naphthyl)-3-oxo-spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3′-oxo-N-[(3S)-5-oxo-1-phenyl-3-pyrrolidinyl]spiro-[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[(3S)-1-(2-fluorophenyl)-3-pyrrolidinyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H), 1′-cyclohexane]-4′-carboxamide, trans-N-[(3S)-1-(3-fluorophenyl)-3-pyrrolidinyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H), 1′-cyclohexane]-4′-carboxamide, trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[7-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3-oxo-N-[(3S)-1-phenyl-3-pyrrolidinyl]spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3-oxo-N-[(3S)-1-(3-trifluoromethylphenyl)-3-pyrrolidinyl]spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3-oxo-N-[(3S)-1-(2-pyridyl)-3-pyrrolidinyl]spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3-oxo-N-[(3S)-1-(3-pyridyl)-3-pyrrolidinyl]spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, -trans-N-[trans-4-(4-fluorophenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxospiro[4-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxospiro[7-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[(3S)-1-(3,5-difluorophenyl)-3-pyrrolidinyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H), 1′-cyclohexane]-4′-carboxamide, trans-N-[1-(3,5-difluorophenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[3-(3-fluorophenyl)-tetrahydropyran-6-yl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[trans-4-(2-fluorophenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-benzyl-2-(benzylamino)ethyl]-3′-oxospiro-[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-benzhydryl-3′-oxospiro[cyclohexane-1,1′(3′H)-iso-benzofuran]-4-carboxamide, trans-1-methanesulfonyl-N-(1-phenyl-4-piperidyl)spiro-[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-(2-indanyl)-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[1-(3-fluorophenyl)-4-piperidyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-[1-(2-pyridyl)-4-piperidyl]spiro-[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-(1-phenyl-3-piperidyl)spiro-[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[1-(3,5-difluorophenyl)-3-piperidyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-[1-(2-pyridyl)-3-piperidyl]spiro-[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-[(3S)-1-phenyl-3-pyrrolidinyl]-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-[(3R)-1-phenyl-3-pyrrolidinyl]-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-(2-phenylcyclopropyl)spiro-[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-[2-(3-pyridyl)cyclopropyl]spiro-[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-benzyl-2-(benzylamino)ethyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[l-benzylcarbamoyl-2-(4-pyridyl)ethyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[2-(4-fluorophenyl)-1-[(4-pyridylmethyl)carbamoyl]-ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-(2-hydroxy-2-phenylethyl)-1-methanesulfonylspiro-[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-(benzoylmethyl)-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-benzyl-2-(N-benzylmethylamino)ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-(N-benzylmethylcarbamoyl)-2-phenylethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-(N-benzylmethylcarbamoyl)-2-(3-pyridyl)-ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-(4-dimethylaminophenethyl)-1-methanesulfonylspiro-[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-[2-(3-quinolyl)ethyl]spiro-[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[2-(4-dimethylaminophenyl)-2-hydroxyethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[2-hydroxy-2-(3-quinolyl)ethyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[2-(3,5-difluorophenyl)-2-hydroxyethyl]-1-methane-sulfonylspiro[sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-benzyl-2-[(3-pyridylmethyl)amino]ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-benzyl-2-[(2-pyridylmethyl)amino]ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-2-anilino-1-benzylethyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-benzyl-2-(isobutylamino)ethyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-[2-phenyl-1-(methoxycarbonyl)-ethyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-(1-hydroxymethyl-2-phenylethyl)-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, 1-methanesulfonyl-N-(1-phenyl-4-piperidyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide, 3-oxo-N-(l-phenyl-3-piperidyl)spiro[isobenzofuran-1(3H),4′-piperidine]-1′-carboxamide, 3-oxo-N-[(3S)-1-phenyl-3-pyrrolidinyl]spiro[isobenzofuran-1(3H),4′-piperidine]-1′-carboxamide, N-[1-benzylcarbamoyl-2-cyclohexylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide, N-[(S)-1-benzyloxymethyl-2-cyclohexylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide, N-[(S)-1-benzylcarbamoyl-2-phenylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide, N-[(S)-1-benzyl-2-(benzylamino)ethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide, N-(2-indanyl)-1-methanesulfonylspiro[indoline-3,4′-piperidine]-1′-carboxamide, 1-methanesulfonyl-N-phenethylspiro[indoline-3,4′-piperidine]-1′-carboxamide, 1-methanesulfonyl-N-(3-phenylpropyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide, 1-methanesulfonyl-N-(4-phenylbutyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide, N-(4-bromophenethyl)-1-methanesulfonylspiro[indoline-3,4′-piperidine]-1′-carboxamide, N-(3,4-dimethoxyphenethyl)-1-methanesulfonylspiro[indoline-3,4′-piperidine]-1′-carboxamide, 1-methanesulfonyl-N-(3-methoxyphenethyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide, N-(4-dimethylamino-2-methoxyphenethyl)-1-methanesulfonyl-spiro[indoline-3,4′-piperidine]-1′-carboxamide, N-[(S)-1-benzyloxycarbonyl-2-(3-indolyl)ethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide, N-[(R)-1-benzyloxycarbonyl-2-(3-indolyl)ethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide, N-[(S)-1-benzyloxycarbonyl-2-cyclohexylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide, 3,4-dihydro-N-(3-methoxyphenethyl)-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide, trans-N-[1-(3-trifluoromethylphenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[trans-2-(3-fluorophenyl)cyclopropyl]-3′-oxospiro-[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[trans-2-(4-fluorophenyl)cyclopropyl]-3′-oxospiro-[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[1-(2-fluorophenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3′-oxo-N-[5-oxo-1-(2-fluorophenyl)-3-pyrrolidinyl]-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-3′-oxo-N-[5-oxo-1-(3-fluorophenyl)-3-pyrrolidinyl]-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-3-oxo-N-[5-oxo-1-(3-fluorophenyl)-3-pyrrolidinyl]-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[trans-4-(3-trifluoromethylphenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3′-oxo-N-[2-oxo-1-phenyl-4-piperidyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-3′-oxo-N-[2-oxo-1-(3-fluorophenyl)-4-piperidyl]spiro-[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[trans-2-(2-fluorophenyl)cyclopropyl]-3′-oxospiro-[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[trans-2-(3-fluorophenyl)cyclopropyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide or trans-N-[trans-2-(4-fluorophenyl)cyclopropyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, and the like.

[0159] The processes for producing the compounds of the present invention are illustrated below.

[0160] The compounds (I) of the present invention can be prepared, for example, by the following production processes or the methods shown in Examples, but Manufacturing methods of the compounds (I) of the present invention are not limited to these embodiments.

[0161] Production Process 1

[0162] A compound of the formula (II):

[0163] (wherein

[0164] A^(p) is a straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of di-lower alkylamino, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl, —R^(ap), optionally protected oxo, optionally protected amino, optionally protected lower alkylamino and optionally protected hydroxy, and is optionally intervened by oxygen or nitrogen atom;

[0165] Ar^(1p) is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, lower alkyl, halo-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, di-lower alkylamino, lower alkylthio, lower alkanoyl, lower alkoxycarbonyl, -Q^(p)-Ar^(2p), optionally protected oxo, optionally protected hydroxy-lower alkyl, optionally protected lower alkylamino and optionally protected carboxyl;

[0166] Ar^(2p) is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, lower alkoxy, halo-lower alkoxy, di-lower alkylamino, lower alkanoyl, aryl, optionally protected hydroxy-lower alkyl, optionally protected hydroxy and optionally protected lower alkylamino;

[0167] Ar³ is phenyl which is optionally substituted by halogen or nitro;

[0168] Q^(p) is a single bond or optionally protected carbonyl;

[0169] R^(ap) is lower alkyl which is optionally substituted by a substituent selected from the group consisting of di-lower alkylamino, optionally protected amino, optionally protected lower alkylamino, optionally protected hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine;

[0170] R^(0p) is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A^(P)) is reacted with a compound of the formula (III):

[0171] (wherein t, u, v and w are independently methine or nitrogen atom, said methine being optionally substituted by a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy and optionally protected hydroxy, and at least two of t, u, v and w are said methine group; n, X and Y have the same meaning as defined above), to provide a compound of the formula (IV-1):

[0172] (wherein A^(p), Ar^(1p), n, R^(0p), t, u, v, w, X and Y have the same meaning as defined above), optionally followed by removal of the protecting group(s) from the compound (IV-1), thereby a compound of the formula (I-1):

[0173] (wherein A, Ar¹, n, R⁰, T, U, V, W, X and Y have the same meaning as defined above) can be prepared.

[0174] The present process is a process for preparing a compound of the formula (I) wherein Z is nitrogen atom, that is, a compound of the formula (I-1).

[0175] In the above reaction, when a reactant has an amino, hydroxy, carboxyl, oxo, carbonyl or the like which does not participate in the reaction, the reaction may be carried out after protecting said amino, hydroxy, carboxyl, oxo or carbonyl with an amino-protecting group, a hydroxy-protecting group, a carboxyl-protecting group, or an oxo- or carbonyl-protecting group, and said protecting groups may be removed after completion of the reaction.

[0176] The “amino-protecting group” includes, for example, aralkyl (e.g. benzyl, p-methoxybenzyl, 3,4-dimethoxybenzyl, o-nitrobenzyl, p-nitrobenzyl, benzhydryl, trityl); lower alkanoyl (e.g. formyl, acetyl, propionyl, butyryl, pivaloyl); benzoyl; arylalkanoyl (e.g. phenylacetyl, phenoxyacetyl); lower alkoxycarbonyl (e.g. methoxycarbonyl, ethoxycarbonyl, propyloxycarbonyl, tert-butoxycarbonyl); aralkyloxycarbonyl (e.g. benzyloxycarbonyl, p-nitrobenzyloxycarbonyl, phenethyloxycarbonyl); lower alkylsilyl (e.g. trimethylsilyl, tert-butyldimethylsilyl); among which the preferred examples are acetyl, pivaloyl, benzoyl, ethoxycarbonyl, tert-butoxycarbonyl, and the like.

[0177] The “hydroxy-protecting group” includes, for example, lower alkyl (e.g. methyl, ethyl, propyl, isopropyl, tert-butyl); lower alkylsilyl (e.g. trimethylsilyl, tert-butyldimethylsilyl); lower alkoxymethyl (e.g. methoxymethyl, 2-methoxyethoxymethyl); tetrahydropyranyl; trimethylsilylethoxymethyl; aralkyl (e.g. benzyl, p-methoxybenzyl, 2,3-dimethoxybenzyl, o-nitrobenzyl, p-nitrobenzyl, trityl); acyl (e.g. formyl, acetyl); among which the preferred examples are methyl, methoxymethyl, tetrahydropyranyl, trityl, trimethylsilylethoxymethyl, tert-butyldimethylsilyl, acetyl, and the like.

[0178] The “carboxyl-protecting group” includes, for example, lower alkyl (e.g. methyl, ethyl, propyl, isopropyl, tert-butyl); halo-lower alkyl (e.g. 2,2,2-trichloroethyl); lower alkenyl (e.g. 2-propenyl); aralkyl (e.g. benzyl, p-methoxybenzyl, p-nitrobenzyl, benzhydryl, trityl), among which the preferred examples are methyl, ethyl, tert-butyl, 2-propenyl, benzyl, p-methoxybenzyl, benzhydryl, and the like.

[0179] The “oxo- or carbonyl-protecting group” includes, for example, acetal (e.g. ethylene ketal, trimethylene ketal, dimethyl ketal), ketal, and the like.

[0180] The reaction between a compound of the formula (II) and a compound of the formula (III) is usually carried out by employing equivalent to excess moles, preferably equivalent to 1.5 moles of the compound of the formula (III) based on 1 mole of the compound (II).

[0181] The reaction is usually carried out in an inert solvent, and preferable examples of such inert solvent are methylene chloride, chloroform, tetrahydrofuran, dimethylformamide, dimethylsulfoxide, etc., or a mixture thereof and the like.

[0182] It is preferable to carry out the above reaction in the presence of a base, and examples of such base are organic bases (e.g. triethylamine, diisopropylethylamine, pyridine, 4-dimethylaminopyridine) or inorganic bases (e.g. sodium hydroxide, potassium hydroxide).

[0183] The amount of the said base employed is usually equivalent to excess moles, preferably 1 to 5 moles based on 1 mole of a compound of the formula (II).

[0184] The reaction temperature is usually from −30° C. to 200° C., preferably from 20° C. to 100° C.

[0185] The reaction time is usually from 5 minutes to 7 days, preferably from 30 minutes to 24 hours.

[0186] Usual workup procedures are applied after completion of the reaction to obtain a crude product of a compound of the formula (IV-1). The resulting compound of the formula (IV-1) is, with or without purification according to the common method, subjected to, if desired, proper combination of removal of the protecting group(s) for amino, hydroxy, carboxyl, oxo and carbonyl, thereby a compound of the formula (I-1) can be prepared.

[0187] Although the method for the removal of said protecting groups depends upon the kinds of the protecting groups, the stability of a desired compound (I-1), etc., it is carried out by, for example, a solvolysis using an acid or a base, that is, for example a method wherein 0.01 mole to a large excess of an acid, preferably trifluoroacetic acid, formic acid, hydrochloric acid and the like, or equivalent moles to a large excess of base, preferably potassium hydroxide, calcium hydroxide and the like is acted; a chemical reduction using a metal hydride complex; or a catalytic reduction using a palladium-carbon catalyst, a Raney-nickel catalyst, etc., according to, for example, a method described in the literature (Protective Groups in Organic Synthesis, T. W. Greene, John Wiley & Sons, (1981)) or its similar methods.

[0188] Production Process 2

[0189] A compound of the formula (V):

[0190] (wherein A^(p), Ar^(1p) and R^(0p) have the same meaning as defined above) is reacted with a carboxylic acid of the formula (VI):

[0191] (wherein n, t, u, v, w, X and Y have the same meaning as defined above) or a reactive derivative thereof to provide a compound of the formula (IV-2):

[0192] (wherein A^(p), Ar^(1p), n, R^(0p), t, u, v, w, X and Y have the same meaning as defined above), optionally followed by removal of the protecting group (s) from the compound (IV-2), thereby a compound of the formula (I-2):

[0193] (wherein A, Ar¹, n, R⁰, T, U, V, W, X and Y have the same meaning as defined above) can be prepared.

[0194] The present process is a process for preparing a compound of the formula (I) wherein Z is methine group, that is, a compound of the formula (I-2).

[0195] The reaction between a compound of the formula (V) and a carboxylic acid of the formula (VI) is usually carried out by employing 0.5 to excess moles, preferably 1 mole to 1.5 moles of the carboxylic acid of the formula (VI) based on 1 mole of the compound of the formula (V).

[0196] The reaction is usually carried out in an inert solvent, and the preferable examples of such inert solvent are methylene chloride, chloroform, tetrahydrofuran, dimethylformamide, pyridine, etc., or a mixture thereof and the like.

[0197] It is preferable to carry out the above reaction in the presence of a condensing agent, and examples of such condensing agent are, N,N′-dicyclohexylcarbodiimide, N,N′-diisopropylcarbodiimide, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, benzotriazol-1-yloxy-tris-(dimethylamino)phosphonium-hexafluorophosphate, benzotriazol-1-yloxy-tris-pyrrolidinophosphonium-hexafluorophosphate, bromotris-(dimethylamino)phosphonium-hexafluorophosphate, diphenylphosphoryl azide, 1,1′-carbonyldiimidazole, and the like.

[0198] The amount of said condensing agent employed may be usually 1 mole to excess mole, preferably 1 to 1.5 moles based on 1 mole of a compound of the formula (VI).

[0199] The reaction temperature is usually from −50° C. to 100° C., preferably from −20° C. to 50° C.

[0200] The reaction time is usually from 30 minutes to 7 days, preferably from 1 hour to 24 hours.

[0201] A compound of the formula (I-2) is also produced by reacting a compound of the formula (V) with an activated derivative of the carboxylic acid of the formula (VI) instead of the carboxylic acid of the formula (VI).

[0202] Examples of the activated derivatives of carboxylic acid of the formula (VI) include acid halides, mixed anhydrides, activated esters, activated amides, and the like.

[0203] The acid halides of carboxylic acid of the formula (VI) may be obtained by reacting a carboxylic acid of the formula (VI) with a halogenating agent according to the conventional method. The halogenating agent includes, for example, thionyl chloride, phosphorus trichloride, phosphorus pentachloride, phosphorus oxychloride, phosphorus tribromide, oxalyl chloride, phosgene, and the like.

[0204] The mixed anhydrides of carboxylic acid of the formula (VI) may be obtained by reacting a carboxylic acid of the formula (VI) with an alkyl chlorocarbonate such as ethyl chlorocarbonate, etc.; an aliphatic carboxylic acid chloride such as pivaloyl chloride, etc., and the like according to the conventional method.

[0205] The activated esters of carboxylic acid of the formula (VI) may be obtained by reacting a carboxylic acid of the formula (VI) with an N-hydroxy compound such as N-hydroxysuccinimide, N-hydroxyphthalimide, 1-hydroxybenzotriazole, etc.; a phenol compound such as 4-nitrophenol, 2,4-dinitrophenol, 2,4,5-trichlorophenol, pentachlorophenol, etc., and the like in the presence of a condensing agent such as N,N′-dicyclohexylcarbodiimide, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide, etc. according to the conventional method.

[0206] The activated amides of carboxylic acid of the formula (VI) may be obtained by reacting a carboxylic acid of the formula (VI) with, for example, 1,1′-carbonyldiimidazole, 1,1′-carbonylbis(2-methylimidazole) according to the conventional method.

[0207] The reaction between a compound of the formula (V) and an activated derivative of carboxylic acid of the formula (VI) is usually carried out by employing 0.5 to excess moles, preferably 1 to 1.5 moles of the activated derivative of carboxylic acid of the formula (VI) based on 1 mole of the compound of the formula (V).

[0208] The reaction is usually carried out in an inert solvent, and the preferable examples of such inert solvent are methylene chloride, chloroform, tetrahydrofuran, dimethylformamide, pyridine, etc., or a mixture thereof and the like.

[0209] Although the above reaction proceeds in the absence of a base, it is preferred to carry out the reaction in the presence of a base to promote the reaction smoothly.

[0210] Examples of such a base are organic bases (e.g. triethylamine, diisopropylethylamine, pyridine, 4-dimethylaminopyridine) or inorganic bases (e.g. sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, sodium hydrogen carbonate).

[0211] The preferable amount of said base is usually 1 to excess moles based on 1 mole of a compound of the formula (V). Also, when the base is a liquid, such base can also be used as a solvent.

[0212] The reaction temperature is usually from −50° C. to 100° C., preferably from −20° C. to 50° C.

[0213] The reaction time is usually from 5 minutes to 7 days, preferably from 30 minutes to 24 hours.

[0214] A compound of the formula (I-2) can be produced by working up the resulting product in the usual way after removal of the said protecting group(s) when the product has a protecting group after completion of the reaction, or by working up the resulting product directly in the usual way when the protecting group is absent.

[0215] The removal of the protecting group(s) and the workup procedure may be carried out according to the method described in the above Production Process 1.

[0216] The compound of the formula (I-1) or (I-2) may be readily isolated and purified by the conventional separation technique, and examples of such technique are solvent extraction, recrystallization, column chromatography, preparative thin layer chromatography and the like.

[0217] These compounds can be converted into the pharmaceutically acceptable salts or esters by the conventional method, and on the contrary, the conversion of the salts or esters into free compounds can also be carried out according to the conventional method.

[0218] Compounds of the formula (II), (III), (V) or (VI) is commercially available, or can be prepared according to the methods described in the literatures (Japanese Patent Unexamined Publication No.94/263737-A, U.S. Pat. No.3,301,857, J. Org. Chem, 40, p.1427 (1975), International Patent Publication W095/28389 and the like), or analogous methods thereto or the methods shown below or in Examples, optionally in combination.

[0219] Production Process A

[0220] In the above reaction scheme, L is halogen; A^(p), Ar^(1p), Ar³ and R^(0p) have the same meaning as defined above.

[0221] The present process is a process for preparing a compound of the formula (II). According to the present process, the compound of the formula (II) can be prepared by reacting a compound of the formula (V) with a compound of the formula 1.

[0222] The reaction between the compound of the formula (V) and the compound of the formula 1 is usually carried out by employing 0.5 to excess moles, preferably equivalent to 1.5 moles of the compound of the formula 1, based on 1 mole of the compound (V).

[0223] The reaction is usually carried out in an inert solvent, and the preferable examples of such inert solvent are methylene chloride, chloroform, tetrahydrofuran, ethyl ether, benzene, toluene, dimethylformamide, etc., or a mixture thereof and the like.

[0224] The above reaction is preferably carried out in the presence of a base, and examples of such base are organic bases (e.g. triethylamine, diisopropylethylamine, pyridine, 4-dimethylaminopyridine) or inorganic bases (e.g. sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, sodium hydrogen carbonate).

[0225] The preferable amount of said base is usually equivalent to excess moles based on 1 mole of a compound of the formula (V). Also, when the base is a liquid, such base can also be used as a solvent.

[0226] The reaction temperature is usually from −78° C. to 100° C., preferably from −20° C. to 50° C.

[0227] The reaction time is usually from 5 minutes to 7 days, preferably from 30 minutes to 24 hours.

[0228] A compound of the formula 1 is commercially available, or can be prepared according to the known methods or the methods in Examples, or analogous methods thereto, optionally in combination.

[0229] The utility of compounds of the present invention as a medicament is proved by showing NPY antagonistic activities in the following pharmacological test.

[0230] Pharmacological Test (NPY Binding Inhibition Test)

[0231] A sequence coding for human NPY Y5 receptor (c.f. International patent publication number W096/16542) was cloned into expression vectors pcDNA3, pRc/RSV (made by Invitrogen Inc.) and pCI-neo (made by Promega Inc.). The expression vectors thus obtained were transfected to host cells COS-7, CHO and LM(tk-) (American Type Culture Collection) by cationic lipid method (Proceedings of the National Academy of Sciences of the United States of America, vol.84: p.7413(1987)) to give NPY Y5 receptor expression cells.

[0232] A membrane sample prepared from the cells which expressed NPY Y5 receptor was incubated together with a test compound and [¹²⁵I]peptideYY (made by NEN) (20,000 cpm) in an assay buffer (25 mM Tris buffer, pH 7.4, containing 10 mM magnesium chloride, 1 mM phenylmethylsulfonyl fluoride, 0.1% bacitracin and 0.5% bovine serum albumin) at 25° C. for 2 hours, then filtered through a glass filter GF/C and washed with 5 mM Tris buffer (pH 7.4) containing 0.3% BSA. The radioactivity of the cake on the glass filter was measured. Non-specific binding was measured in the presence of 1 μM peptide YY, and 50% Inhibitory Concentration (IC₅₀) of the test compound against specific peptideYY binding was determined (Endocrinology, vol.131: p.2090(1992)). The results are shown in Table 1. TABLE 1 NPY receptors binding inhibition compounds IC₅₀ (nM) Example 1 2.5 Example 5 1.7 Example 27 3.6 Example 32 1.7 Example 36 0.80 Example 41 1.2 Example 45 0.69 Example 46 2.0

[0233] As shown above, the compounds of this invention potently inhibited peptideYY (NPY analogue) binding to NPY Y5 receptors.

[0234] The compounds of the formula (I) can be administered orally or parenterally and, by formulating into a suitable administrable form, may be administered as a therapeutic agent for various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, etc., sexual and reproductive dysfunctions, gastro-intestinal disorders such as gastro-intestinal motility disorder, respiratory disorders, inflammatory diseases or glaucoma, and the like, particularly preferably bulimia, obesity, diabetes, and the like. In clinical use, the compounds of this invention may be administered after being formulated, together with pharmaceutically acceptable additives, into an appropriate preparation according to the mode of administration. As for such additives, those which are usually used in the field of pharmaceutical formulation, for example, gelatin, lactose, sucrose, titanium oxide, starch, crystalline cellulose, hydroxypropyl methylcellulose, carboxymethylcellulose, corn starch, microcrystalline wax, white petrolatum, magnesium methasilicate aluminate, anhydrous calcium phosphate, citric acid, trisodium citrate, hydroxypropyl cellulose, sorbitol, sorbitan fatty acid ester, polysorbate, sucrose fatty acid ester, polyoxyethylene, hydrogenated castor oil, polyvinylpyrrolidone, magnesium stearate, light silicic anhydride, talc, vegetable oil, benzyl alcohol, gum arabic, propylene glycol, polyalkylene glycol, cyclodextrin or hydroxypropyl cyclodextrin, etc. may be used.

[0235] The formulations prepared by mixing the compound of the present invention with said additives include, for example, solid preparations (e.g. tablets, capsules, granules, powder, suppositories); or liquid preparations (e.g. syrups, elixirs, injections). Such preparations may be formulated according to the techniques well-known in the art of pharmaceutical formulation. Liquid preparations may be in the form of preparations which are dissolved or suspended in water or other appropriate media when used. In the case of injectable preparations in particular, they may be dissolved or suspended in physiological saline or glucose solution if necessary, optionally together with a buffer or a preservative.

[0236] All the said preparations may contain 1.0 to 100 wt. %, preferably 1.0 to 60 wt. % of compounds of the present invention and may also contain other therapeutically effective compounds.

[0237] The compounds of the present invention can be used in combination with other agents useful for treating metabolic disorders and/or eating disorders. The individual component of such combinations can be administered separately at different times or concurrently in divided or single combination forms during the course of therapy. The present invention is therefore to be understood as embracing all such regimes of simultaneous or divided administration and the term “administration” is to be interpreted accordingly. The scope of combinations of the compounds of this invention with other agents useful for treating metabolic disorders and/or eating disorders includes in principle any combination of any pharmaceutical composition useful for treating metabolic disorders and/or eating disorders.

[0238] When compounds of the present invention are used clinically, for example, a daily dose for an adult is 0.01 to 100 mg/kg, preferably 0.03 to 3 mg/kg with simultaneous or divided administration when administered orally, and 0.001 to 10 mg/kg, preferably 0.001 to 0.1 mg/kg with simultaneous or divided administration when administered parenterally, though the dose and the frequency of administration may vary depending upon the sex, age, body weight, degree of symptoms, and type and range of the desired treatment effects.

[0239] An ordinarily skilled physician, veterinarian or clinician can readily determine and prescribe the effective amount of the drug required to prevent, suppress or arrest the progress of diseases.

BEST MODE FOR CARRYING OUT THE INVENTION

[0240] The present invention is further described in detail with reference to the following Examples, but the invention should in no way be restricted thereby.

EXAMPLE 1 Preparation of trans-3′-oxo-N-(trans-4-phenylcyclohexyl)-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0241] 4-Phenylcyclohexylamine hydrochloride (64 mg) and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (115 mg) were added to a solution of trans-3′-oxospiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-caboxylic acid (74 mg) in pyridine (2 mL). The mixture was stirred at room temperature for 24 hours and the reaction mixture was partitioned between water and ethyl acetate. The organic layer was dried over magnesium sulfate and the solvent was removed by evaporation. The residue was purified by preparative thin-layer chromatography (hexane/ethyl acetate=1/1) to give the title compound (50.7 mg) as a white solid.

[0242]¹H-NMR (300 MHz, CDCl₃, δppm): 1.72-1.89 (2H, m), 1.56-1.82 (4H, m), 1.92-2.20 (8H, m), 2.28-2.40 (2H, m), 2.45-2.58 (2H, m), 3.82-3.96 (1H, m), 5.44 (1H, br d), 7.17-7.33 (5H, m), 7.52 (1H, d, J=7.8 Hz), 7.58-7.69 (2H, m), 7.88 (1H, d, J=7.5 Hz).

[0243] Compounds of Examples 2 to 76 were obtained by following the same procedure as in Example 1, except that trans-3′-oxospiro[cyclohexan-1,1′(3′H)-isobenzofuran]-4-carboxylic acid and 4-phenylcyclohexylamine hydrochloride used in Example 1 were replaced with the corresponding starting materials of each desired compound.

EXAMPLE 2 Trans-N-[(3S)-1-(2-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0244]¹H-NMR(300 MHz,DMSO-d₆,δppm): 1.69-1.77 (2H,m), 1.83-2.18 (8H,m), 2.47-2.53 (1H,m), 3.17-3.23 (1H,m), 3.28-3.34 (1H,m), 3.43-3.47 (1H,m), 3.55-3.62 (1H,m), 4.35-4.38 (1H,m), 6.65-6.76 (2H,m), 6.97-7.08 (2H,m), 7.58-7.64 (2H,m), 7.77 (1H,d,J=7.3Hz), 7.83 (1H,d,J=7.6Hz), 8.17 (1H,d,J=6.9Hz).

EXAMPLE 3 Trans-N-[(3S)-1-(3-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0245]¹H-NMR(300 MHz,CDCl₃,δppm): 1.74-1.80 (2H,m), 2.00-2.15 (5H,m), 2.23-2.38 (3H,m), 2.48-2.52 (1H,m), 3.20 (1H,dd,J=9.9,3.6 Hz), 3.35-3.47 (2H,m), 3.59-3.65 (1H,m), 4.66-4.68 (1H,m), 5.73-5.77 (1H,m), 6.23-6.45 (3H,m), 7.17 (1H,dt,J=8.2,6.9 Hz), 7.49-7.58 (2H,m), 7.63-7.69 (1H,m), 7.87 (1H,dd,J=7.6, 0.8 Hz).

EXAMPLE 4 Trans-N-[(3S)-1-(4-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0246]¹H-NMR(300 MHz,CDCl₃,δppm): 1.74-1.82 (2H,m), 1.99-2.39 (8H,m), 2.48-2.52 (1H,m), 3.19 (1H,dd,J=9.9, 3.3 Hz), 3.26-3.34 (1H,m), 3.41-3.48 (1H,m), 3.56 (1H,dd,J=9.9, 5.9 Hz), 4.65-4.72 (1H,m), 5.77-5.80 (1H,m), 6.48-6.54 (2H,m), 6.93-7.00 (2H,m), 7.49-7.58 (2H,m), 7.62-7.68 (1H,m), 7.88 (1H,dd,J=7.6, 0.9 Hz).

EXAMPLE 5 Trans-N-[1-(2-fluorophenyl)-4-piperidyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0247]¹H-NMR(300 MHz,CD₃OD,δppm): 1.80-1.92 (2H,m), 1.99-2.37 (10H,m), 2.60-2.70 (1H,m), 3.71-3.89 (4H,m), 4.04-4.20 (1H,m), 7.37-7.50 (2H,m), 7.52-7.64 (2H,m), 7.69-7.89 (4H,m).

EXAMPLE 6 Trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0248]¹H-NMR(300 MHz,CD₃OD,δppm): 1.78-1.92 (2H,m), 1.98-2.38 (10H,m), 2.59-2.69 (1H,m), 3.67-3.88 (4H,m), 4.07-4.20 (1H,m), 7.28 (1H,dt,J=7.6,1.5 Hz), 7.43-7.68 (4H,m), 7.70-7.79 (2H,m), 7.84 (1H,d,J=7.6 Hz).

EXAMPLE 7 Trans-N-[1-(4-fluorophenyl)-4-piperidyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0249]¹H-NMR(300 MHz,CD₃OD,δppm): 1.77-1.93 (2H,m), 1.98-2.41 (10H,m), 2.60-2.71 (1H,m), 3.70-3.91 (4H,m), 4.11-4.26 (1H,m), 7.30-7.43 (2H,m), 7.55-7.66 (1H,m), 7.71-7.81 (2H,m), 7.81-7.94 (3H,m).

EXAMPLE 8 Trans-3′-oxo-N-(1,2,3,4-tetrahydro-2-naphthyl)spiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0250]¹H-NMR(300 MHz,CDCl₃,δppm): 1.70-1.91 (3H,m), 1.96-2.19 (5H,m), 2.19-2.39 (2H,m), 2.49 (1H,q,J=5.0 Hz), 2.73 (1H,dd,J=16.3, 7.9 Hz), 2.79-3.03 (2H,m), 3.15 (1H,dd,J=16.3, 5.0 Hz), 4.37-4.42 (1H,m), 5.62 (1H,br d,J=7.6 Hz), 6.99-7.21 (4H,m), 7.46-7.70 (3H,m), 7.86 (1H,dd,J=7.6, 1.0 Hz).

EXAMPLE 9 Trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[4-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0251]¹H-NMR(300 MHz,CDCl₃,δppm): 1.61 (2H,dq,J=11.6, 4.0 Hz), 1.70-1.95 (2H,m), 1.95-2.23 (6H,m), 2.23-2.45 (2H,m), 2.53 (1H,quintet,J=5.1 Hz), 2.81-3.03 (2H,m), 3.65 (2H,brd,J=12.9 Hz), 3.90-4.07 (1H,m), 5.72 (1H,brd,J=7.7 Hz), 6.52 (1H,dt,J=8.2, 2.3 Hz),6.58 (1H,dt,J=12.3, 2.3 Hz), 6.69 (1H,dt,J=8.3, 2.3 Hz), 7.17 (1H,q,J=7.9 Hz), 7.56 (1H,dd,J=7.3, 4.6 Hz), 8.03 (1H,d,J=7.9 Hz), 8.89 (1H,d,J=4.6 Hz).

EXAMPLE 10 Trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0252]¹H-NMR(300 MHz,CDCl₃,δppm): 1.59 (2H,dq,J=11.5, 4.0 Hz),1.70-2.60 (8H,m), 2.80-3.03 (2H,m), 3.55-3.79 (2H,m), 3.90-4.09 (1H,m), 5.63 (1H,brd,J=7.9 Hz), 6.30-6.81 (3H,m), 7.10-7.24 (1H,m), 7.59 (1H,dd,J=5.2, 1.2 Hz), 8.84 (1H,d,J=5.2 Hz), 9.14 (1H,s).

EXAMPLE 11 Trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0253]¹H-NMR(300 MHz,CDCl₃,δppm): 1.50-1.70 (2H,m), 1.70-1.96 (2H,m), 1.96-2.27 (6H,m), 2.27-2.61 (3H,m), 2.82-3.02 (2H,m), 3.57-3.78 (2H,m), 3.94-4.09 (1H,m), 5.64 (1H,brd,J=7.9 Hz), 6.44-6.78 (3H,m), 7.10-7.23 (1H,m), 7.77 (1H,dd,J=5.0, 1.1 Hz), 8.86 (1H,d,J=5.0 Hz), 9.04 (1H,d,J=1.1 Hz).

Example 12 Trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[7-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0254]¹H-NMR(300 MHz,CDCl₃,δppm): 1.49-1.69 (2H,m), 1.80-2.53 (11H,m), 2.82-3.03 (2H,m), 3.53-3.78 (2H,m), 3.95-4.17 (1H,m), 5.70 (1H,br d,J=7.6 Hz), 6.43-6.76 (3H,m), 7.11-7.24 (1H,m), 7.49 (1H,dd,J=7.8, 4.9 Hz), 8.15 (1H,dd,J=7.8, 1.6 Hz), 8.84 (1H,dd,J=4.9, 1.6 Hz).

EXAMPLE 13 Trans-N-(6-methoxy-1,2,3,4-tetrahydro-2-naphthyl)-3-oxospiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0255]¹H-NMR(300 MHz,CDCl₃,δppm): 1.71-1.95 (3H,m), 1.95-2.23 (5H,m), 2.23-2.42 (2H,m), 2.50 (1H,q,J=5.0 Hz), 2.66 (1H,dd,J=16.0, 7.8 Hz), 2.77-3.01 (2H,m), 3.07 (1H,dd,J=16.0,5.0 Hz), 3.77 (3H,s), 4.24-4.42 (1H,m), 5.96 (1H,br d,J=7.7 Hz), 6.65 (1H,d,J=2.5 Hz), 6.72 (1H,dd, J=8.4, 2.5 Hz), 6.97 (1H,d,J=8.5 Hz), 7.61 (1H,d, J=5.0 Hz), 8.83 (1H,d,J=5.0 Hz), 9.12 (1H,s).

EXAMPLE 14 Trans-3′-oxo-N-[(3S)-5-oxo-1-phenyl-3-pyrrolidinyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0256]¹H-NMR(300 MHz,DMSO-d₆,δppm): 1.68-1.76 (2H,m), 1.86-2.11 (6H,m), 2.40-2.54 (2H,m), 2.92 (1H,dd,J=17.1, 8.2 Hz), 3.60-3.67 (1H,m), 4.16 (1H,dd,J=10.2, 7.0 Hz), 4.46-4.51 (1H,m), 7.10-7.16 (3H,m), 7.33-7.40 (2H,m), 7.57-7.67 (4H,m), 7.74-7.84 (2H,m), 8.46 (1H,d,J=6.7 Hz).

EXAMPLE 15 Trans-N-[(3S)-1-(2-fluorophenyl)-3-pyrrolidinyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0257]¹H-NMR(300 MHz,CDCl₃,δppm): 1.80-2.00 (3H,m), 2.00-2.20 (4H,m), 2.30-2.40 (3H,m), 2.52 (1H,quintet,J=5.2 Hz), 3.30-3.40 (2H,m), 3.50-3.70 (2H,m), 4.60-4.70 (1H,m), 5.94 (1H,d,J=7.7 Hz), 6.65-6.80 (2H,m), 6.95-7.10 (2H,m), 7.70-7.80 (1H,m), 8.86 (1H,d,J=4.9 Hz), 9.04 (1H,s).

EXAMPLE 16 Trans-N-[(3S)-1-(3-fluorophenyl)-3-pyrrolidinyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0258]¹H-NMR(300 MHz,CDCl₃,δppm): 1.75-1.90 (2H,m), 2.00-2.20 (5H,m), 2.30-2.40 (3H,m), 2.51 (1H,quintet,J=4.9 Hz), 3.20 (1H,dd,J=10.2, 3.4 Hz), 3.30-3.50 (2H,m), 3.61 (1H,dd,J=10.0, 6.0 Hz), 4.60-4.70 (1H,m), 5.93 (1H,d,J=7.2 Hz), 6.25 (1H,dt,J=12.1, 2.3 Hz), 6.30-6.36 (1H,m), 6.36-6.45 (1H,m), 7.15 (1H,dt,J=8.2, 6.9 Hz), 7.70-7.80 (1H,m), 8.80-8.90 (1H,m), 9.04 (1H,s).

EXAMPLE 17 Trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0259]¹H-NMR(300 MHz,CDCl₃,δppm): 1.18-1.93 (2H,m), 1.49-1.74 (2H,m), 1.72-1.88 (2H,m), 1.91-2.22 (8H,m), 2.27-2.42 (2H,m), 2.45-2.59 (2H,m), 3.79-3.97 (1H,m), 5.33-5.48 (1H,m), 7.12-7.35 (5H,m), 7.58 (1H,d,J=5.4 Hz), 8.84 (1H,d,J=5.4 Hz), 9.15 (1H,s).

EXAMPLE 18 Trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0260]¹H-NMR(300 MHz,CDCl₃,δppm): 1.15-1.41 (2H,m), 1.43-1.84 (2H,m), 1.86-2.24 (10H,m), 2.28-2.60 (4H,m), 3.78-4.00 (1H,m), 5.29-5.50 (1H,m), 7.08-7.37 (5H,m), 7.76 (1H,dd,J=4.8, 1.2 Hz), 8.86 (1H,d,J=4.8 Hz), 9.04 (1H,d,J=1.2 Hz).

EXAMPLE 19 Trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[7-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0261]¹H-NMR(300 MHz,CDCl₃,δppm): 1.18-1.43 (2H,m), 1.43-1.77 (2H,m), 1.77-2.62 (14H,m), 3.80-4.00 (1H,m), 5.34-5.51 (1H,m), 7.09-7.48 (5H,m), 7.46 (1H,dd,J=7.8, 4.8 Hz), 8.17 (1H,dd,J=7.8, 1.5 Hz), 8.84 (1H,dd,J=4.8, 1.5 Hz).

EXAMPLE 20 Trans-3-oxo-N-[(3S)-1-phenyl-3-pyrrolidinyl]spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0262]¹H-NMR(300 MHz,CDCl₃,δppm): 1.75-1.88 (2H,m), 1.95-2.20 (6H,m), 2.30-2.54 (4H,m), 3.20-3.62 (4H,m), 4.62-4.72 (1H,m), 5.70-5.80 (1H,m), 6.60 (2H,d,J=8.7 Hz), 6.74 (1H,t,J=7.4 Hz), 7.20-7.32 (2H,m), 7.76 (1H,d,J=5.0 Hz), 8.87 (1H,d,J=5.0 Hz), 9.04 (1H,s).

EXAMPLE 21 Trans-3-oxo-N-[(3S)-1-(3-trifluoromethylphenyl)-3-pyrrolidinyl]spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0263]¹H-NMR(200 MHz,CDCl₃,δppm): 1.75-2.57 (11H,m), 3.18-3.71 (4H,m), 4.62-4.78 (1H,m), 5.68-5.80 (1H,m), 6.68-6.80 (2H,m), 6.90-7.00 (1H,m), 7.25-7.38 (1H,m), 7.76 (1H,d,J=5.0 Hz), 8.87 (1H,d,J=5.0 Hz), 9.04 (1H,s).

EXAMPLE 22 Trans-3-oxo-N-[(3S)-1-(2-pyridyl)-3-pyrrolidinyl]spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0264]¹H-NMR(300 MHz,CDCl₃,δppm): 1.70-1.90 (2H,m), 2.00-2.20 (5H,m), 2.20-2.40 (3H,m), 2.51 (1H,quintet,J=4.9 Hz), 3.00-3.10 (2H,m), 3.42 (1H,dd,J=10.9, 3.6 Hz), 3.77 (1H,dd,J=10.9, 5.9 Hz), 4.60-4.70 (1H,m), 5.83 (1H,d,J=7.3 Hz), 6.38 (1H,d,J=8.6 Hz), 6.55-6.65 (1H,m), 7.64 (1H,ddd,J=9.0,7.0,2.0 Hz), 7.56 (1H,dd,J=5.4, 1.6 Hz), 8.10-8.20 (1H,m), 8.84 (1H,d,J=5.4 Hz), 9.14 (1H,s).

EXAMPLE 23 Trans-3-oxo-N-[(3S)-1-(3-pyridyl)-3-pyrrolidinyl]spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0265] H-NMR(300 MHz,CDCl₃,δppm): 1.70-1.90 (2H,m), 2.00-2.20 (5H,m), 2.25-2.45 (3H,m), 2.54 (1H,quintet,J=5.3 Hz), 3.23 (1H,dd,J=9.9, 3.0 Hz), 3.30-3.50 (2H,m), 3.63 (1H,dd,J=9.7, 5.9 Hz), 4.60-4.70 (1H,m), 6.17 (1H,d,J=7.2 Hz), 6.70-6.90 (1H,m), 7.00-7.20 (1H,m), 7.57 (1H,dd,J=5.3, 0.9 Hz), 7.90-8.00 (2H,m), 8.85 (1H,d,J=5.3 Hz), 9.15 (1H,s).

EXAMPLE 24 Trans-N-[trans-4-(4-fluorophenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0266]¹H-NMR(300 MHz,CDCl₃,δppm): 1.13-1.41 (2H,m), 1.41-1.68 (2H,m), 1.72-2.26 (10H,m), 2.26-2.60 (4H,m), 3.78-4.00 (1H,m), 5.32-5.51 (1H,m), 6.81-7.07 (2H,m), 7.07-7.37 (2H,m), 7.76 (1H,dd,J=5.4, 1.2 Hz), 8.86 (1H,d,J=5.4 Hz), 9.04 (1H,d,J=1.2 Hz).

EXAMPLE 25 Trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0267]¹H-NMR(300 MHz,CDCl₃,δppm): 1.19-1.41 (2H,m), 1.49-1.73 (2H,m), 1.73-2.27 (10H,m), 2.39-2.70 (4H,m), 3.79-4.00 (1H,m), 5.32-5.48 (1H,m), 6.82-7.03 (3H,m), 7.19-7.34 (1H,m), 7.76 (1H,dd,J=4.8, 0.9 Hz), 8.86 (1H,d,J=4.8 Hz), 9.04 (1H,d,J=0.9 Hz).

EXAMPLE 26 Trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxospiro[4-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0268]¹H-NMR(300 MHz,CDCl₃,δppm): 1.19-1.41 (2H,m), 1.49-1.73 (2H,m), 1.73-2.25 (10H,m), 2.25-2.42 (2H,m), 2.42-2.60 (2H,m), 3.77-3.96 (1H,m), 5.36-5.56 (1H,m), 6.82-7.03 (1H,m), 7.19-7.34 (1H,m), 7.54 (1H,dd,J=7.8, 4.5 Hz), 8.03 (1H,d,J=7.8 Hz), 8.88 (1H,d,J=4.5 Hz).

EXAMPLE 27 Trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxospiro[7-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0269]¹H-NMR(300MHz,CDCl₃,δppm): 1.19-1.41 (2H,m), 1.49-1.76 (2H,m), 1.78-2.60 (14H,m), 3.80-4.00 (1H,m), 5.35-5.53 (1H,m), 6.82-7.03 (3H,m), 7.18-7.35 (1H,m), 7.46 (1H,dd,J=7.8, 4.8 Hz), 8.17 (1H,dd,J=J=7.8, 1.5 Hz), 8.84 (1H,dd,J=4.8, 1.5 Hz).

EXAMPLE 28 Trans-N-[(3S)-1-(3,5-difluorophenyl)-3-pyrrolidinyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0270]¹H-NMR(300 MHz,CDCl₃,δppm): 1.80-1.90 (2H,m), 1.95-2.20 (5H,m), 2.30-2.45 (3H,m), 2.53 (1H,quintet,J=4.6 Hz), 3.10-3.20 (1H,m), 3.30-3.50 (2H,m), 3.60-3.70 (1H,m), 4.60-4.70 (1H,m), 5.60-5.70 (1H,m), 6.50-6.60 (2H,m), 6.60-6.70 (1H,m), 7.76 (1H,d,J=4.9 Hz), 8.87 (1H,d,J=4.9 Hz), 9.03 (1H,s).

EXAMPLE 29 Trans-N-[1-(3,5-difluorophenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0271]¹H-NMR(300 MHz,CDCl₃,δppm): 1.45-1.61 (2H,m), 1.78-1.90 (2H,m), 2.00-2.21 (6H,m), 2.31-2.45 (2H,m), 2.45-2.55 (1H,m), 2.88-3.00 (2H,m), 3.60-3.71 (2H,m), 3.95-4.10 (1H,m), 5.48 (1H,br d,J=7.5 Hz), 6.18-6.29 (1H,m), 6.29-6.43 (2H,m), 7.77 (1H,dd,J=5.0, 1.1 Hz), 8.86 (1H,d,J=5.0 Hz), 9.03 (1H,d,J=1.1 Hz).

EXAMPLE 30 Trans-N-[3-(3-fluorophenyl)-tetrahydropyran-6-yl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0272]¹H-NMR(300 MHz,CDCl₃,δppm): 1.43-2.10 (13H,m), 3.24 (1H,t,J=10.5 Hz), 4.02-4.20 (1H,m), 4.24 (1H,d,J=10.5 Hz), 4.32 (1H,d,J=10.5 Hz), 5.20-5.40 (1H,m), 6.88-7.03 (1H,m), 7.03-7.16 (2H,m), 7.20-7.39 (1H,m), 7.76 (1H,dd,J=5.1, 1.2 Hz), 8.87 (1H,d,J=5.1Hz), 9.04 (1H,d,J=1.2 Hz).

EXAMPLE 31 Trans-N-[trans-4-(2-fluorophenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0273]¹H-NMR(300 MHz,CDCl₃,δppm): 1.22-1.46 (2H,m), 1.52-2.28 (12H,m), 2.28-2.60 (3H,m), 2.76-2.97 (1H,m), 3.80-4.00 (1H,m), 5.35-5.53 (1H,m), 6.92-7.41 (4H,m), 7.76 (1H,dd,J=4.8, 1.2 Hz), 8.86 (1H,d,J=4.8 Hz), 9.04 (1H,d,J=1.2 Hz).

EXAMPLE 32 Trans-N-[(S)-1-benzyl-2-(benzylamino)ethyl]-3′-oxospiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4′-carboxamide

[0274]¹H-NMR(300 MHz,CDCl₃,δppm): 1.50-1.74 (2H,m), 1.60-2.10 (5H,m), 2.16-2.27 (1H,m), 2.39-2.47 (1H,m), 2.68-2.75 (2H,m), 2.86 (2H,d,J=6.6 Hz), 3.79 (2H,s), 4.28-4.39 (1H,m), 5.85 (1H,d,J=8.4 Hz), 7.13-7.37 (10H,m), 7.46 (1H,d,J=8.1 Hz), 7.51 (1H,d,J=7.8 Hz), 7.63 (1H,t,J=7.8 Hz), 7.86 (1H,d,J=7.8 Hz).

EXAMPLE 33 Trans-N-benzhydryl-3′-oxospiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0275]¹H-NMR(200 MHz,CDCl₃,δppm): 1.70-1.80 (2H,m), 2.10-2.40 (6H,m), 2.64 (1H,quintet,J=4.9 Hz), 6.16 (1H,d,J=7.6 Hz), 6.28 (1H,d,J=7.6 Hz), 7.20-7.40 (10H,m), 7.45-7.55 (2H,m), 7.60-7.70 (1H,m), 7.80-7.90 (1H,m).

EXAMPLE 34 Trans-1-methanesulfonyl-N-(1-phenyl-4-piperidyl)spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0276]¹H-NMR(300 MHz,CDCl₃,δppm): 1.50-1.70 (4H,m), 1.71-1.83 (2H,m), 1.95-2.15 (6H,m), 2.30-2.40 (1H,m), 2.82-2.96 (2H,m), 2.89 (3H,s), 3.60-3.68 (2H,br d,J=12.9 Hz), 3.72 (2H,s), 3.92-4.08 (1H,m), 5.47 (1H,d,J=7.7 Hz), 6.85 (1H,t,J=7.3 Hz), 6.94 (2H,d,J=8.5 Hz), 7.05 (1H,t,J=7.3 Hz), 7.18-7.30 (3H,m), 7.40 (2H,t,J=7.3 Hz).

EXAMPLE 35 Trans-N-(2-indanyl)-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0277]¹H-NMR(300 MHz,CDCl₃,δppm): 1.50-1.63 (2H,m), 1.68-1.80 (2H,m), 1.99-2.11 (4H,m), 2.23-2.32 (1H,m), 2.81 (2H,dd,J=16.2, 4.2 Hz), 2.88 (3H,s), 3.36 (2H,dd,J=16.2, 7.2 Hz), 3.70 (2H,s), 4.72-4.85 (1H,m), 5.68-5.77 (1H,m), 7.05 (1H,t,J=7.2 Hz), 7.18-7.30 (5H,m), 7.34-7.45 (2H,m).

EXAMPLE 36 Trans-N-[1-(3-fluorophenyl)-4-piperidyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0278]¹H-NMR(300 MHz,CDCl₃,δppm): 1.46-1.68 (4H,m), 1.70-1.84 (2H,m), 2.00-2.13 (6H,m), 2.30-2.40 (1H,m), 2.89 (3H,s), 2.86-2.98 (2H,m), 3.61-3.71 (2H,m), 3.72 (2H,s), 3.95-4.05 (1H,m), 5.43 (1H,d,J=7.7 Hz), 6.49 (1H,dt,J=8.2, 2.3 Hz), 6.60 (1H,dt,J=12.4, 2.3 Hz), 6.68 (1H,dd,J=8.2, 2.3 Hz), 7.05 (1H,dt,J=7.6, 1.1 Hz), 7.17 (1H,t,J=7.6 Hz), 7.22 (1H,dt,J=7.6, 1.3 Hz), 7.40 (1H,dd,J=7.6, 1.1 Hz), 7.42 (1H,dd,J=7.6, 1.1 Hz).

EXAMPLE 37 Trans-1-methanesulfonyl-N-[1-(2-pyridyl)-4-piperidyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0279]¹H-NMR(300 MHz,CDCl₃,δppm): 1.38-1.54 (2H,m), 1.53-1.63 (2H,m), 1.65-1.75 (4H,m), 2.00-2.12 (6H,m), 2.29-2.40 (1H,m), 2.88 (3H,s), 3.02 (2H,ddd,J=13.8, 11.2, 2.5 Hz), 3.72 (2H,s), 4.06 (1H,m), 4.25 (2H,m), 5.44 (1H,d,J=7.8 Hz), 6.56-6.66 (1H,m), 6.68 (1H,d,J=8.7 Hz), 7.05 (1H,dt,J=7.6, 1.0 Hz), 7.22 (1H,dt,J=7.6, 1.2 Hz), 7.39 (1H,d,J=7.6 Hz), 7.42 (1H,dd,J=7.6, 1.0 Hz), 7.47 (1H,ddd,J=8.8, 7.1, 2.0 Hz), 8.13-8.24 (1H,m).

EXAMPLE 38 Trans-1-methanesulfonyl-N-(1-phenyl-3-piperidyl)spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0280]¹H-NMR(300 MHz,CDCl₃,δppm): 1.54-1.88 (8H,m), 2.00-2.19 (4H,m), 2.33-2.42 (1H,m), 2.89 (3H,s), 2.96-3.05 (1H,m), 3.13-3.43 (3H,m), 3.68-3.75 (2H,m), 4.20-4.30 (1H,m), 6.03-6.10 (1H,m), 6.88 (1H,t,J=7.2 Hz), 6.91-6.99 (2H,m), 7.01-7.08 (1H,m), 7.19-7.30 (3H,m), 7.37-7.43 (2H,m).

EXAMPLE 39 Trans-N-[1-(3,5-difluorophenyl)-3-piperidyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0281]¹H-NMR(300 MHz,CDCl₃,δppm): 1.53-1.90 (8H,m), 2.00-2.13 (4H,m), 2.33-2.42 (1H,m), 2.88 (3H,s), 3.01-3.20 (3H,m), 3.40-3.48 (1H,m), 3.67-3.82 (2H,m), 4.10-4.21 (1H,m), 5.97-6.03 (1H,m), 6.19-6.28 (1H,m), 6.35-6,45 (2H,m), 7.05 (1H,t,J=7.5 Hz), 7.22 (1H,t,J=7.5 Hz), 7.38 (1H,d,J=7.8 Hz), 7.42 (1H,d,J=7.8 Hz).

EXAMPLE 40 Trans-1-methanesulfonyl-N-[1-(2-pyridyl)-3-piperidyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0282]¹H-NMR(300 MHz,CDCl₃,δppm): 1.50-1.90 (8H,m), 1.95-2.32 (4H,m), 2.31-2.40 (1H,m), 2.88 (3H,s), 3.43-3.50 (1H,m), 3.70 (2H,s), 3.55-3.74 (3H,m), 4.08-4.16 (1H,m), 6.30 (1H,d,J=7.6 Hz), 6.61 (1H,dd,J=7.1, 5.0 Hz), 6.73 (1H,d,J=8.6 Hz), 7.03 (1H,dt,J=7.5, 1.1 Hz), 7.21 (1H,dt,J=7.5, 1.1Hz), 7.38 (2H,d,J=8.6 Hz), 7.47 (1H,ddd,J=8.6, 7.1, 2.0 Hz), 8.14 (1H,dd,J=5.0, 2.0 Hz).

EXAMPLE 41 Trans-1-methanesulfonyl-N-[(3S)-1-phenyl-3-pyrrolidinyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0283]¹H-NMR(300 MHz,CDCl₃,δppm): 1.52-1.82 (6H,m), 1.96-2.13 (3H,m), 2.28-2.40 (2H,m), 2.87 (3H,m), 3.22 (1H,dd,J=9.9, 3.3 Hz), 3.31-3.51 (2H,m), 3.59 (1H,dd,J=9.9, 5.7 Hz), 3.67-3.72 (2H,m), 4.61-4.71 (1H,m), 5.82-5.89 (1H,m), 6.60 (2H,d,J=7.8 Hz), 6.73 (1H,t,J=7.5 Hz), 7.04 (1H,dd,J=7.5, 1.2 Hz), 7.20-7.29 (3H,m), 7.40 (2H,t,J=8.4 Hz).

EXAMPLE 42 Trans-1-methanesulfonyl-N-[(3R)-1-phenyl-3-pyrrolidinyl spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0284]¹H-NMR(300 MHz,CDCl₃,δppm): 1.52-1.82 (6H,m), 1.96-2. 13 (3H,m), 2.28-2.40 (2H,m), 2.87 (3H,m), 3.22 (1H,dd,J=9.9, 3.3 Hz), 3.31-3.51 (2H,m), 3.59 (1H,dd,J=9.9, 5.7 Hz), 3.67-3.72 (2H,m), 4.61-4.71 (1H,m), 5.82-5.89 (1H,m), 6.60 (2H,d,J=7.8 Hz), 6.73 (1H,t,J=7.5 Hz), 7.04 (1H,dd,J=7.5, 1.2 Hz), 7.20-7.29 (3H,m), 7.40 (2H,t,J=8.4 Hz).

EXAMPLE 43 Trans-1-methanesulfonyl-N-(2-phenylcyclopropyl)spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0285]¹H-NMR(300 MHz,CDCl₃,δppm): 1.10-1.30 (2H,m), 1.50-1.87 (4H,m), 1.95-2.20 (5H,m), 2.30-2.38 (1H,m), 2.89 (3H,s), 2.86-2.95 (1H,m), 3.72 (2H,s), 5.75-5.84 (1H,m), 6.99-7.48 (9H,m).

EXAMPLE 44 Trans-1-methanesulfonyl-N-[2-(3-pyridyl)cyclo-propyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0286]¹H-NMR(300 MHz,CDCl₃,δppm): 1.20-1.34 (2H,m), 1.52-1.89 (4H,m), 2.00-2.20 (5H,m), 2.34-2.43 (1H,m), 2.89 (3H,s), 2.87-2.94 (1H,m), 3.72 (2H,s), 5.86-5.95 (1H,m), 7.05 (1H,dt,J=7.5, 1.1 Hz), 7.19-7.30 (2H,m), 7.37-7.47 (2H,m), 7.51 (1H,brd,J=7.9 Hz), 8.45 (1H,dd,J=4.7 Hz, 1.7 Hz), 8.50 (1H,d,J=2.1 Hz).

EXAMPLE 45 Trans-N-[(S)-1-benzyl-2-(benzylamino)ethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0287]¹H-NMR(300 MHz,CDCl₃,δppm): 1.46-1.75 (4H,m), 1.82-2.05 (4H,m), 2.25-2.34 (1H,m), 2.68-2.72 (2H,m), 2.88 (3H,s), 2.80-2.90 (2H,m), 3.70 (2H,s), 3.77 (2H,s), 4.25-4.36 (1H,m), 5.85 (1H,d,J=7.5 Hz), 7.03 (1H,t,J=7.5 Hz), 7.15-7.32 (12H,m), 7.38 (1H,d,J=7.5 Hz).

EXAMPLE 46 Trans-N-[1-benzylcarbamoyl-2-(4-pyridyl)ethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0288]¹H-NMR(300 MHz,CDCl₃,δppm): 1.45-2.02 (8H,m), 2.30-2.40 (1H,m), 2.88 (3H,s), 3.00-3.19 (2H,m), 3.68 (2H,s), 4.28-4.43 (2H,m), 4.78 (1H,q,J=7.5 Hz), 6.40-6.52 (2H,m), 6.98-7.40 (11H,m), 8.46 (2H,d,J=5.9 Hz).

EXAMPLE 47 Trans-N-[2-(4-fluorophenyl)-1-[(4-pyridyl-methyl)carbamoyl]ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0289]¹H-NMR(300 MHz,CDCl₃,δppm): 1.45-2.10 (8H,m), 2.35-2.45 (1H,m), 2.88 (3H,s), 3.00-3.18 (2H,m), 3.70 (2H,s), 4.31 (1H,dd,J=15.8, 6.0 Hz), 4.41 (1H,dd,J=15.8, 6.0 Hz), 4.76 (1H,q,J=7.9 Hz), 6.42 (1H,d,J=7.9 Hz), 6.79 (1H,t,J=6.0 Hz), 6.90-7.10 (5H,m), 7.11-7.32 (4H,m), 7.38 (1H,d,J=8.0 Hz), 8.47 (2H,d,J=5.3 Hz).

EXAMPLE 48 Trans-N-(2-hydroxy-2-phenylethyl)-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0290]¹H-NMR(300 MHz,CDCl₃,δppm): 1.50-1.63 (2H,m), 1.67-1.82 (2H,m), 1.92-2.12 (4H,m), 2.33-2.42 (1H,m), 2.89 (3H,s), 3.27-3.47 (2H,m), 3.71 (2H,s), 3.72-3.82 (1H,m), 4.88-4.94 (1H,m), 5.91-6.02 (1H,m), 7.05 (1H,t,J=7.8 Hz), 7.19-7.41 (8H,m).

EXAMPLE 49 Trans-N-(benzoylmethyl)-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0291]¹H-NMR(300 MHz,CDCl₃,δppm): 1.59-1.70 (2H,m), 1.80-1.91 (2H,m), 2.02-2.21 (4H,m), 2.51-2.60 (1H,m), 2.90 (3H,s), 3.76 (2H,s), 4.81 (2H,d,J=4.2 Hz), 6.60-6.70 (1H,m), 7.04 (1H,t,J=7.5 Hz), 7.22 (1H,t,J=7.5 Hz), 7.38-7.43 (2H,m), 7.52 (2H,t,J=7.5 Hz), 7.64 (1H,t,J=7.5 Hz), 8.00 (2H,d,J=6.6 Hz).

EXAMPLE 50 Trans-N-[(S)-1-benzyl-2-(N-benzylmethylamino)ethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0292]¹H-NMR(300 MHz,CDCl₃,δppm): 1.50-1.78 (4H,m), 1.80-2.10 (4H,m), 2.23 (3H,s), 2.28-2.46 (3H,m), 2.88 (3H,s), 2.92 (2H,d,J=6.6 Hz), 3.46 (1H,d,J=13.2 Hz), 3.53 (1H,d,J=13.2 Hz), 3.71 (2H,s), 4.25-4.38 (1H,m), 5.62 (1H,d,J=6.6 Hz), 7.02 (1H,t,J=7.5 Hz), 7.12-7.34 (12H,m), 7.38 (1H,d,J=7.5 Hz).

EXAMPLE 51 Trans-N-[(S)-1-(N-benzylmethylcarbamoyl)-2-phenylethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0293]¹H-NMR(300 MHz,CDCl₃,δppm): 1.45-2.10 (8H,m), 2.33-2.46 (1H,m), 2.75 (3H,s), 2.88 (3H,s), 3.00-3.10 (2H,m), 3.69 (2H,s), 4.46 (1H,d,J=14.4 Hz), 4.63 (1H,d,J=14.4 Hz), 5.20-5.35 (1H,m), 6.75 (1H,d,J=7.5 Hz), 7.00-7.36 (13H,m), 7.39 (1H,d,J=7.5 Hz).

EXAMPLE 52 Trans-N-[(S)-1-(N-benzylmethylcarbamoyl)-2-(3-pyridyl)ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0294]¹H-NMR(300 MHz,CDCl₃,δppm): 1.45-2.08 (8H,m), 2.30-2.45 (1H,m), 2.88 (3H,s), 2.97 (3H,s), 2.95-3.02 (1H,m), 3.12 (1H,dd,J=13.6, 7.2 Hz), 3.70 (2H,s), 4.45-4.62 (2H,m), 5.20-5.30 (1H,m), 6.60 (1H,br s), 7.00-7.48 (11H,m), 8.45 (1H,d,J=1.8 Hz), 8.47 (1H,dd,J=5.1, 1.8 Hz).

EXAMPLE 53 Trans-N-(4-dimethylaminophenethyl)-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0295]¹H-NMR(300 MHz,CDCl₃,δppm): 1.49-1.80 (4H,m), 1.94-2.09 (4H,m), 2.22-2.33 (1H,m), 2.75 (2H,t,J=6.6 Hz), 2.88 (3H,s), 2.92 (6H,s), 3.52 (2H,dt,J=6.6, 6.2 Hz), 3.70 (2H,s), 5.51 (1H,t,J=6.2 Hz), 6.70 (2H,d,J=8.8 Hz), 7.04 (1H,t,J=8.1 Hz), 7.07 (2H,d,J=8.8 Hz), 7.22 (1H,t,J=8.1 Hz), 7.39 (2H,d,J=8.1 Hz).

EXAMPLE 54 Trans-1-methanesulfonyl-N-[2-(3-quinolyl)ethyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0296]¹H-NMR(300 MHz,CDCl₃,δppm): 1.49-1.79 (4H,m), 1.92-2.09 (4H,m), 2.25-2.36 (1H,m), 2.88 (3H,s), 3.07 (2H,t,J=6.6 Hz), 3.65 (1H,dt,J=6.7, 6.6 Hz), 3.69 (1H,dd,J=6.7, 6.6 Hz), 3.69 (2H,s), 5.63 (1H,t,J=6.7 Hz), 7.02 (1H,t,J=7.3 Hz), 7.22 (1H,t,J=7.3 Hz), 7.33 (1H,d,J=7.3 Hz), 7.38 (1H,d,J=7.3 Hz), 7.54 (1H,t,J=7.9 Hz), 7.69 (1H,t,J=7.9 Hz), 7.77 (1H,d,J-7.9 Hz), 7.99 (1H,d,J=2.2 Hz), 8.08 (1H,d,J=7.9 Hz), 8.79 (1H,d,J=2.2 Hz).

EXAMPLE 55 Trans-N-[2-(4-dimethylaminophenyl)-2-hydroxyethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0297]¹H-NMR(300 MHz,CDCl₃,δppm): 1.49-1.82 (4H,m), 1.98-2.12 (4H,m), 2.32-2.42 (1H,m), 2.63-2.70 (1H,m), 2.89 (3H,s), 2.94 (6H,s), 3.35-3.45 (1H,m), 3.71 (2H,s), 3.60-3.78 (1H,m), 4.72-4.80 (1H,s), 5.90-5.98 (1H,m), 6.65-6.75 (2H,m), 7.00-7.09 (1H,m), 7.18-7.30 (3H,m), 7.35-7.45 (2H,m).

EXAMPLE 56 Trans-N-[2-hydroxy-2-(3-quinolyl)ethyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0298]¹H-NMR(300 MHz,CDCl₃,δppm): 1.50-1.82 (4H,m), 1.92-2.10 (4H,m), 2.32-2.45 (1H,m), 2.88 (3H,s), 3.48-3.60 (2H,m), 3.69 (2H,s), 3.82-3.95 (1H,m), 4.19-4.30 (1H,m), 5.12-5.20 (1H,m), 7.04 (1H,t,J=7.8 Hz), 7.23 (1H,t,J=7.8 Hz), 7.33 (1H,d,J=7.8 Hz), 7.38 (1H,d,J=7.8 Hz), 7.55 (1H,t,J=7.8 Hz), 7.71 (1H,t,J=7.8 Hz), 7.80 (1H,d,J=7.8 Hz), 8.10 (1H,d,J=7.8 Hz), 8.21 (1H,d,J=2.4 Hz), 8.88 (1H,d,J=2.4 Hz).

EXAMPLE 57 Trans-N-[2-(3,5-difluorophenyl)-2-hydroxyethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0299]¹H-NMR(300 MHz,CDCl₃,δppm): 1.51-2.32 (4H,m), 1.94-2.01 (4H,m), 2.35-2.46 (1H,s), 2.89 (3H,s), 3.31-3.42 (1H,m), 3.71 (2H,s), 3.70-3.82 (1H,m), 3.98 (1H,d,J=4.3 Hz), 4.87-4.94 (1H,m), 5.98 (1H,t,J=3.0 Hz), 6.68-6.76 (1H,m), 6.87-6.98 (2H,m), 7.06 (1H,t,J=7.7 Hz), 7.23 (1H,t,J=7.7 Hz), 7.32-7.41 (2H,m).

EXAMPLE 58 Trans-N-[(S)-1-benzyl-2-[(3-pyridylmethyl)amino]ethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0300]¹H-NMR(300 MHz,CDCl₃,δppm): 1.45-1.75 (4H,m), 1.80-2.09 (4H,m), 2.25-2.38 (1H,m), 2.70 (2H,d,J=7.5 Hz), 2.86 (3H,s), 2.84-2.90 (2H,m), 3.69 (2H,s), 3.78 (2H,s), 4.25-4.40 (1H,m), 5.70 (1H,d,J=7.5 Hz), 7.03 (1H,dd,J=7.5, 2.4 Hz), 7.12-7.40 (9H,m), 7.57-7.63 (1H,m), 8.50 (1H,dd,J=5.1, 1.5 Hz), 8.55 (1H,d,J=1.5 Hz).

EXAMPLE 59 Trans-N-[(S)-1-benzyl-2-[(2-pyridylmethyl)amino]ethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0301]¹H-NMR(300 MHz,CDCl₃,δppm): 1.45-2.10 (8H,m), 2.30-2.40 (1H,m), 2.66-2.76 (2H,m), 2.88 (3H,s), 2.80-2.99 (2H,m), 3.70 (2H,s), 3.90 (2H,dd,J=14.4, 5.7 Hz), 4.23-4.37 (1H,m), 6.14 (1H,d,J=7.5 Hz), 7.02 (1H,t,J=7.5 Hz), 7.12-7.30 (9H,m), 7.36 (1H,t,J=7.5 Hz), 7.62 (1H,dt,J=7.5, 2.1 Hz), 8.54 (1H,dd,J=5.1, 2.1 Hz).

EXAMPLE 60 Trans-N-[(S)-2-anilino-1-benzylethyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0302]¹H-NMR(300 MHz,CDCl₃,δppm): 1.42-2.07 (8H,m), 2.24-2.33 (1H,m), 2.87 (3H,s), 2.84-2.91 (1H,m), 3.00 (1H,dd,J=14.1, 6.3 Hz), 3.20 (1H,dd,J=12.4, 7.5 Hz), 3.33 (1H,dd,J=12.4, 4.5 Hz), 3.67 (2H,s), 4.47-4.58 (1H,m), 5.49 (1H,d,J=7.5 Hz), 6.60 (1H,d,J=7.5 Hz), 6.70 (1H,t,J=7.5 Hz), 7.00 (1H,t,J=7.5 Hz), 7.12-7.40 (10H,m).

EXAMPLE 61 Trans-N-[(S)-1-benzyl-2-(isobutylamino)ethyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0303]¹H-NMR(300 MHz,CDCl₃,δppm): 0.89 (6H,d,J=6.3 Hz), 1.45-2.10 (9H,m), 2.30-2.40 (1H,m), 2.43 (2H,d,J=6.3 Hz), 2.65-2.78 (2H,m), 2.88 (3H,s), 2.80-2.93 (2H,m), 3.70 (2H,s), 4.22-4.35 (1H,m), 6.02 (1H,d,J=7.5 Hz), 7.15-7.40 (9H,m).

EXAMPLE 62 Trans-1-methanesulfonyl-N-[2-phenyl-1-(methoxy-carbonyl)ethyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0304]¹H-NMR(300 MHz,CDCl₃,δppm): 1.49-1.60 (2H,m), 1.63-1.78 (2H,m), 1.87-2.10 (4H,m), 2.33-2.41 (1H,m), 2.88 (3H,s), 3.10 (1H,dd,J=14.1, 6.3 Hz), 3.22 (1H,dd,J=14.1, 5.7 Hz), 3.71 (2H,s), 3.77 (3H,s), 4.91-4.97 (1H,m), 5.95 (1H,br d,J=7.8 Hz), 7.04 (1H,t,J=6.9 Hz), 7.11 (2H,d,J=6.3 Hz), 7.19-7.40 (6H,m).

EXAMPLE 63 Trans-N-(1-hydroxymethyl-2-phenylethyl)-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

[0305]¹H-NMR(200 MHz,CDCl₃,δppm): 1.43-2.11 (7H,m), 2.29-2.40 (1H,m), 2.52-2.67 (1H,m), 2.79-3.02 (2H,m), 2.88 (3H,s), 3.59-3.81 (2H,m), 3.69 (2H,s), 4.18-4.35 (1H,m), 5.69-5.81 (1H,m), 7.04 (1H,dt,J=7.6, 1.2 Hz), 7.18-7.41 (8H,m).

EXAMPLE 64 Trans-N-[1-(3-trifluoromethylphenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0306]¹H-NMR(300 MHz,CDCl₃,δppm): 1.56-1.65 (2H,m), 1.80-1.88 (2H,m), 2.04-2.21 (6H,m), 2.35-2.44 (2H,m), 2.50-2.53 (1H,m), 2.91-3.00 (2H,m), 3.62-3.73 (2H,m), 4.00-4.16 (1H,m), 5.58-5.60 (1H,m), 7.06-7.13 (3H,m), 7.27-7.37 (4H,m), 7.76 (1H,d,J=3.7Hz), 8.87 (1H,d,J=4.9 Hz), 9.04 (1H,s).

EXAMPLE 65 Trans-N-[trans-2-(3-fluorophenyl)cyclopropyl]-3′-oxospiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0307]¹H-NMR(300 MHz,CDCl₃,δppm): 1.18-1.31 (2H,m), 1.70-1.82 (2H,m), 2.00-2.21 (5H,m), 2.22-2.38 (2H,m), 2.46-2.56 (1H,m), 2.89-2.98 (1H,m), 6.89 (1H,br s), 6.83-6.91 (2H,m), 6.97 (1H,d,J=7.2 Hz), 7.19-7.29 (1H,m), 7.52 (1H,t,J=7.2 Hz), 7.55-7.69 (2H,m), 7.87 (1H,d,J=7.8 Hz).

EXAMPLE 66 Trans-N-[trans-2-(4-fluorophenyl)cyclopropyl]-3′-oxospiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0308]¹H-NMR(300 MHz,CDCl₃,δppm): 1.12-1.28 (2H,m), 1.71-1.82 (2H,m), 1.99-2.20 (5H,m), 2.21-2.38 (2H,m), 2.46-2.54 (1H,m), 2.81-2.90 (1H,m), 5.86 (1H,br s), 6.98 (2H,t,J=8.7 Hz), 7.13-7.21 (2H,m), 7.52 (1H,t,J=7.2 Hz), 7.58-7.70 (2H,m), 7.88 (1H,d,J=7.8 Hz).

EXAMPLE 67 Trans-N-[1-(2-fluorophenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran]-1(3H),1′-cyclohexane]-4′-carboxamide

[0309]¹H-NMR(300 MHz,CDCl₃,δppm): 1.56-1.74 (2H,m), 1.78-1.90 (2H,m), 2.01-2.23 (6H,m), 2.32-2.48 (2H,m), 2.48-2.57 (1H,m), 2.77-2.90 (2H,m), 3.38-3.50 (2H,m), 3.90-4.07 (1H,m), 5.51 (1H,m), 6.90-7.10 (4H,m), 7.74 (1H,d,J=5.0 Hz), 8.87 (1H,d,J=5.0 Hz), 9.05 (1H,s).

EXAMPLE 68 Trans-3′-oxo-N-[5-oxo-1-(2-fluorophenyl)-3-pyrrolidinyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0310]¹H-NMR(300 MHz,CDCl₃,δppm): 1.68-1.81 (2H,m), 1.96-2.15 (4H,m), 2.15-2.30 (2H,m), 2.43-2.54 (2H,m), 2.99 (1H,dd,J=17.4, 7.6 Hz), 3.73 (1H,dd,J=10.6, 2.4 Hz), 4.16 (1H,dd,J=10.6, 6.0 Hz), 4.65-4.76 (1H,m), 6.80 (1H,br s), 7.09-7.21 (2H,m), 7.23-7.32 (1H,m), 7.32-7.42 (1H,m), 7.47-7.57 (2H,m), 7.59-7.68 (1H,m), 7.88 (1H,d,J=7.5 Hz).

EXAMPLE 69 Trans-3′-oxo-N-[5-oxo-1-(3-fluorophenyl)-3-pyrrolidinyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0311]¹H-NMR(300 MHz,CDCl₃,δppm): 1.71-1.94 (2H,m), 2.01-2.34 (6H,m), 2.52-2.64 (2H,m), 2.98-3.11 (1H,m), 3.77 (1H,dd,J=10.5, 2.9 Hz), 4.23 (1H,dd,J=10.5, 6.4 Hz), 4.65-4.77 (1H,m), 6.78-7.13 (2H,m), 7.17-7.33 (2H,m), 7.42-7.69 (4H,m), 7.80-7.88 (1H,m).

EXAMPLE 70 Trans-3-oxo-N-[5-oxo-1-(3-fluorophenyl)-3-pyrrolidinyl]spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0312]¹H-NMR(300 MHz,CDCl₃,δppm): 1.76-1.91 (2H,m), 2.06-2.23 (4H,m), 2.25-2.40 (2H,m), 2.50-2.62 (2H,m), 3.07 (1H,dd,J=17.6, 8.1 Hz), 3.77 (1H,dd,J=10.7, 2.4 Hz), 4.24 (1H,dd,J=10.6, 6.2 Hz), 4.67-4.79 (1H,m), 6.79-6.92 (2H,m), 7.16-7.35 (2H,m), 7.46-7.54 (1H,m), 7.75 (1H,d,J=5.0 Hz), 8.87 (1H,d,J=5.0 Hz), 9.04 (1H,s).

EXAMPLE 71 Trans-N-[trans-4-(3-trifluoromethylphenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0313]¹H-NMR(300 MHz,CDCl₃,δppm): 1.26-1.40 (2H,m), 1.59-1.72 (2H,m), 1.80-1.88 (2H,m), 1.97-2.20 (7H,m), 2.36-2.63 (4H,m), 3.88-3.93 (1H,m), 5.42 (1H,d,J=8.4 Hz), 7.40-7.47 (4H,m), 7.76 (1H,d,J=6.0 Hz), 8.87 (1H,d,J=4.9 Hz), 9.04 (1H,s).

EXAMPLE 72 Trans-3′-oxo-N-[2-oxo-1-phenyl-4-piperidyl]spiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0314]¹H-NMR(300 MHz,CDCl₃,δppm): 1.65-1.85 (1H,m), 1.95-2.20 (5H,m), 2.20-2.40 (3H,m), 2.43-2.60 (2H,m), 2.92-3.00 (1H,m), 3.60-3.80 (2H,m), 4.40-4.45 (1H,m), 5.68-5.70 (1H,m), 7.20-7.23 (3H,m), 7.38-7.42 (2H,m), 7.45-7.56 (2H,m), 7.62-7.66 (1H,m), 7.86-7.87 (1H,m).

EXAMPLE 73 Trans-3′-oxo-N-[2-oxo-1-(3-fluorophenyl)-4-piperidyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0315]¹H-NMR(300 MHz,CDCl₃,δppm): 1.60-1.90 (1H,m), 1.95-2.20 (5H,m), 2.22-2.60 (5H,m), 2.96-3.00 (1H,m), 3.62-3.80 (2H,m), 4.38-4.50 (1H,m), 5.70-5.80 (1H,m), 7.20-7.30 (4H,m), 7.40-7.42 (2H,m), 7.72-7.80 (1H,m), 8.84-8.85 (1H,m), 9.01 (1H,s).

EXAMPLE 74 Trans-N-[trans-2-(2-fluorophenyl)cyclopropyl]-3′-oxospiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

[0316]¹H-NMR(300 MHz,CDCl₃,δppm): 1.20-1.37 (2H,m), 1.70-1.82 (2H,m), 2.01-2.38 (7H,m), 2.48-2.57 (1H,m), 3.00-3.09 (1H,m), 5.92 (1H,br s), 6.99-7.21 (4H,m), 7.51 (1H,t,J=7.2 Hz), 7.56-7.69 (2H,m), 7.87 (1H,d,J=7.5 Hz).

EXAMPLE 75 Trans-N-[trans-2-(3-fluorophenyl)cyclopropyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0317]¹H-NMR(300 MHz,CDCl₃,δppm): 1.17-1.32 (2H,m), 1.75-1.89 (2H,m), 2.00-2.25 (5H,m), 2.31-2.58 (3H,m), 2.89-2.99 (1H,m), 5.84 (1H,br s), 6.80-7.03 (3H,m), 7.20-7.32 (1H,m), 7.76 ((1H,dd,J=5.1, 0.9 Hz), 8.87 (1H,d,J=5.1 Hz), 9.03 (1H,d,J=0.9 Hz).

EXAMPLE 76 Trans-N-[trans-2-(4-fluorophenyl)cyclopropyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

[0318]¹H-NMR(300 MHz,CDCl₃,δppm): 1.12-1.30 (2H,m), 1.78-1.90 (2H,m), 2.01-2.22 (5H,m), 2.31-2.48 (2H,m), 2.48-2.57 (1H,m), 2.82-2.91 (1H,m), 5.84 (1H,br s), 6.98 (2H,t,J=8.7 Hz), 7.12-7.22 (2H,m), 7.76 (1H,dd,J=4.8, 1.2 Hz), 8.87 (1H,d,J=4.8 Hz), 9.04 (1H,s).

EXAMPLE 77 Preparation of 1-methanesulfonyl-N-(1-phenyl-4-piperidyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide

[0319] (1) Preparation of phenyl N-(1-phenyl-4-piperidyl)carbamate

[0320] Pyridine (24 μL) and phenyl chlorocarbonate (32 μL) were added to a solution of 1-phenyl-4-piperidylamine (35 mg) in tetrahydrofuran (1 mL), and the mixture was stirred at room temperature for 12 hours. The reaction mixture was poured into saturated aqueous sodium bicarbonate, and extracted with ethyl acetate. The organic layer was dried over anhydrous magnesium sulfate and concentrated. The residue was purified by column chromatography on silica gel (ethyl acetate/chloroform=1/1) to give the title compound (37 mg).

[0321] (2) Preparation of 1-methanesulfonyl-N-(1-phenyl-4-piperidyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide

[0322] 1-Methanesulfonyl-spiro[indoline-3,4′-piperidine] hydrochloride (37 mg) and triethylamine (170 μL) were added to a solution of phenyl N-(1-phenyl-4-piperidyl)carbamate (36 mg) in chloroform (3 mL), and the mixture was heated to reflux for 15 hours. The reaction mixture was poured into saturated aqueous sodium bicarbonate and extracted with ethyl acetate. The organic layer was dried over anhydrous magnesium sulfate and concentrated. The residue was crystallized from diethyl ether to give the title compound (18 mg) as a colorless crystal.

[0323]¹H-NMR(300 MHz,CDCl₃,δppm): 1.49-2.13 (12H,m), 2.71-2.83 (1H,m), 2.84-3.00 (2H,m), 2.92 (3H,s), 3.10-3.19 (1H,m), 3.60-3.70 (1H,m), 3.85 (2H,s), 3.90-4.01 (1H,m), 4.37 (1H,d,J=7.8 Hz), 6.84 (1H,t,J=7.2 Hz), 6.94 (1H,d,J=8.7 Hz), 7.07 (1H,t,J=7.2 Hz), 7.11-7.29 (5H, m), 7.40 (1H,d,J=8.4 Hz).

[0324] Compounds of Examples 78 to 83 were obtained by following the same procedure as in Example 77-(2), except that phenyl N-(1-phenyl-4-piperidyl)carbamate and 1-methanesulfonylspiro[indoline-3,4′-piperidine] hydrochloride used in Example 77-(2) were replaced with the corresponding starting material of each desired compound.

EXAMPLE 78 3-Oxo-N-(1-phenyl-3-piperidyl)spiro[isobenzofuran-1(3H),4′-piperidine]-1′-carboxamide

[0325]¹H-NMR(300 MHz,CDCl₃,δppm): 1.60-1.90 (2H,m), 2.04-2.18 (2H,m), 2.53-2.60 (1H,m), 3.01-3.49 (9H,m), 3.92-4.20 (3H,m), 5.03 (1H,d,J=7.8 Hz), 6.88 (1H,t,J=7.5 Hz), 6.97 (2H,d,J=7.5 Hz), 7.21-7.30 (2H,m), 7.35 (1H,d,J=7.8 Hz), 7.54 (1H,t,J=7.5 Hz), 7.68 (1H,t,J=7.5 Hz), 7.88 (1H,d,J=7.5 Hz).

EXAMPLE 79 3-Oxo-N-[(3S)-1-phenyl-3-pyrrolidinyl]spiro[isobenzofuran-1(3H),4′-piperidine]-1′-carboxamide

[0326]¹H-NMR(300 MHz,CDCl₃,δppm): 1.98-2.20 (3H,m) , 2.30-2.41 (1H,m), 2.99-3.10 (2H,m), 3.22-3.40 (4H,m), 3.42-3.53 (1H,m), 3.59-3.65 (1H,m), 3.96-4.11 (2H,m), 4.53-4.64 (1H,m), 4.68-4.77 (1H,m), 6.60 (2H,d,J=7.8 Hz), 6.72 (1H,t,J=7.5 Hz), 7.25 (2H,t,J=7.5 Hz), 7.37 (1H,d,J=7.5 Hz), 7.55 (1H,t,J=7.5 Hz), 7.69 (1H,t,J=7.5 Hz), 7.89 (1H,d,J=7.8 Hz).

EXAMPLE 80 N-[1-Benzylcarbamoyl-2-cyclohexylethyl]-3,4-dihydro-3-oxo-spiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide

[0327]¹H-NMR(300 MHz,CDCl₃,δppm): 0.88-1.03 (2H,m), 1.10-1.25 (3H,m), 1.27-1.45 (1H,m), 1.50-1.86 (8H,m), 2.03-2.19 (2H,m), 3.05-3.19 (2H,m), 3.66 (2H,s), 3.94-4.05 (2H,m), 4.34-4.43 (2H,m), 4.52 (1H,dd,J=13.5, 6.0 Hz), 5.10 (1H,d,J=7.5 Hz), 6.60 (2H,br s), 7.15-7.37 (9H,m).

EXAMPLE 81 N-[(S)-1-Benzyloxymethyl-2-cyclohexylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide

[0328]¹H-NMR(300 MHz,CDCl₃,δppm): 0.80-1.32 (7H,m), 1.40-1.50 (2H,m), 1.60-1.85 (6H,m), 2.03-2.20 (2H,m), 3.02-3.18 (2H,m), 3.47 (1H,dd,J=9.7, 3.3 Hz), 3.54 (1H,dd,J=9.7, 3.3 Hz), 3.66 (2H,s), 3.90-4.02 (2H,m), 4.02-4.17 (1H,m), 4.49 (1H,d,J=12.2 Hz), 4.54 (1H,d,J=12.2 Hz), 4.70 (1H,d,J=8.7 Hz), 6.64 (1H,s), 7.10-7.40 (9H,m).

EXAMPLE 82 N-[(S)-1-Benzylcarbamoyl-2-phenylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide

[0329]¹H-NMR(300 MHz,CDCl₃,δppm): 1.70-1.80 (2H,m), 1.90-2.12 (2H,m), 3.00-3.20 (2H,m), 3.64 (2H,s), 3.83-4.00 (2H,m), 4.30 (1H,dd,J=15.0, 5.7 Hz), 4.39 (1H,dd,J=15.0, 5.7 Hz), 4.58 (1H,dd,J=14.5, 7.5 Hz), 5.37 (1H,d,J=7.5 Hz), 6.31 (1H,br s), 6.73 (1H,br s), 7.08 (2H,dd,J=7.5, 2.4 Hz), 7.13-7.37 (12H,m).

EXAMPLE 83 N-[(S)-1-Benzyl-2-(benzylamino)ethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide

[0330]¹H-NMR(300 MHz,CDCl₃,δppm): 1.60-1.85 (2H,m), 1.93-2.14 (2H,m), 2.68 (2H,d,J=5.4 Hz), 2.77 (1H,dd,J=13.5, 7.5 Hz), 2.97 (1H,dd,J=13.5, 5.4 Hz), 3.02-3.18 (2H,m), 3.65 (2H,s), 3.75 (2H,s), 3.82-4.04 (2H,m), 4.07-4.20 (1H,m), 5.00 (1H,d,J=6.9 Hz), 6.79 (1H,br s), 7.10-7.36 (14H,m).

EXAMPLE 84 Preparation of N-(2-indanyl)-1-methanesulfonyl-spiro[indoline-3,4′-piperidine]-1′-carboxamide

[0331] 1-Methanesulfonylspiro[indoline-3,4′-piperidine]hydrochloride (60 mg) and 10M aqueous sodium hydroxide (33 μL) were added to a solution of phenyl N-(2-indanyl)carbamate (50 mg) in dimethyl sulfoxide (2 mL), and the mixture was stirred at room temperature for one hour. The reaction mixture was poured into water, and extracted with ethyl acetate. The organic layer was dried over anhydrous magnesium sulfate and concentrated. The residue was washed with ethyl acetate to give the title compound (65 mg) as a colorless crystal.

[0332]¹H-NMR(300 MHz,CDCl₃,δppm): 1.72 (2H,d,J=13.9 Hz), 1.83-1.95 (2H, m), 2.81-2.98 (4H,m), 2.91 (3H,s), 3.37 (2H,dd,J=16.4, 6.4 Hz), 3.84 (2H,s), 3.95 (2H,d,J=13.5 Hz), 4.69 (2H,br s), 7.06-7.28 (7H,m), 7.40 (1H,d,J=8.4 Hz).

[0333] Compounds of Examples 85 to 88 were obtained by following the same procedure as in Example 84, except that phenyl N-(2-indanyl)carbamate and 1-methanesulfonylspiro[indoline-3,4′-piperidine] hydrochloride used in Example 84 were replaced with the corresponding starting materials of each desired compound.

EXAMPLE 85 1-Methanesulfonyl-N-phenethylspiro[indoline-3,4′-piperidine]-1′-carboxamide

[0334]¹H-NMR(300 MHz,CDCl₃,δppm): 1.61-1.72 (2H,m), 1.79-1.89 (2H,m), 2.83-2.96 (4H,m), 2.86 (3H,s), 3.83 (2H,s), 3.85-3.94 (2H,m), 4.49 (1H,br s), 7.04-7.41 (9H,m).

EXAMPLE 86 1-Methanesulfonyl-N-(3-phenylpropyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide

[0335]¹H-NMR(300 MHz,CDCl₃,δppm): 1.70-1.77 (2H,m), 1.86-2.02 (2H,m), 2.71 (2H,t,J=7.4 Hz), 2.88-2.99 (2H,m), 2.92 (3H,s), 3.33 (2H,t,J=7.0 Hz), 3.74-3.82 (2H,m), 3.84 (2H,s), 7.08 (1H,t,J=7.4Hz), 7.15-7.32 (8H,m), 7.40 (1H,d,J=7.7 Hz).

EXAMPLE 87 1-Methanesulfonyl-N-(4-phenylbutyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide

[0336]¹H-NMR(300 MHz,CDCl₃,δppm): 1.54-2.00 (8H,m), 2.66 (2H,t,J=7.3 Hz), 2.92 (3H,s), 2.93-3.04 (2H,m), 3.29 (2H,t,J=7.0 Hz), 3.85 (2H,s), 3.86-3.94 (2H,m), 7.07-7.11 (1H,m), 7.15-7.31 (8H,m), 7.38-7.42 (1H,m).

EXAMPLE 88 N-(4-Bromophenethyl)-1-methanesulfonylspiro[indoline-3,4′-piperidine]-1′-carboxamide

[0337]¹H-NMR(300 MHz,DMSO-d₆,δppm): 1.55-1.70 (4H,m), 2.73 (2H,t,J=7.1 Hz), 2.78-2.88 (2H,m), 3.04 (3H,s), 3.22-3.32 (2H,m), 3.87 (2H,s), 3.91 (2H,brd, J=13.2 Hz), 7.06 (1H,t,J=7.2 Hz), 7.18-7.29 (5H,m), 7.48 (2H,d,J=8.2 Hz).

EXAMPLE 89 Preparation of N-(3,4-dimethoxyphenethyl)-1-methane-sulfonylspiro[indoline-3,4′-piperidine]-1′-carboxamide

[0338] 2-(4-Formyl-3-methoxyphenoxy)ethyl polystyrene resin (500 mg), 1% acetic acid-dimethylformamide (10 mL), 2-(3,4-dimethoxyphenyl)ethylamine (236 μL) and sodium triacetoxyborohydride (590 mg) were successively added into a 75 mL-reservoir equipped with a frit. The mixture was stirred at room temperature overnight and then filtered. The remaining resin was washed successively with dimethylformamide, methanol and methylene chloride (10 mL each), and dried under reduced pressure to give 2-[4-[2-(3,4-dimethoxyphenyl)ethyl]amino-methyl-3-methoxyphenoxy]ethyl polystyrene resin. Then, the resin (50 mg) obtained above, methylene chloride (5 mL), triphosgene (22 mg) and triethylamine (38 μL) were added to a 15 mL—reservoir equipped with a frit. The mixture was stirred at room temperature for 6 hours and then filtered. The remaining resin was washed with methylene chloride, and methylene chloride (5 mL), 1-methanesulfonylspiro(indoline-3,4′-piperidine) hydrochloride (22 mg) and triethylamine (77 μL) were added thereto. The mixture was stirred at room temperature overnight and then filtered. The resin thus obtained was washed successively with dimethylformamide, methanol and methylene chloride (10 mL each), and stirred in 50% trifluoroacetic acid-methylene chloride solution for one hour to give a crude product. The product was purified by chromatography on silica gel to give the title compound (7 mg).

[0339]¹H-NMR(300 MHz,CDCl₃,δppm): 1.65-1.75 (2H,m), 1.78-1.93 (2H,m), 2.80 (2H,t,J=6.9 Hz), 2.83-2.98 (2H,m), 2.92 (3H,s), 3.50 (1H,t,J=6.5 Hz), 3.52 (1H,t,J=6,5 Hz), 3.83 (2H,s), 3.86 (3H,s), 3.88 (3H,s), 3.80-3.95 (2H,m), 4.51 (1H,t), 6.71-6.78 (2H,m), 6.79-6.84 (1H,m), 7.03-7.15 (2H,m), 7.20-7.28 (1H,m), 7.40 (1H,d,J=1.8 Hz).

[0340] Compounds of Examples 90 to 95 were obtained by following the same procedure as in Example 89, except that 2-(3,4-dimethoxyphenyl)ethylamine and 1-methanesulfonylspiro[indoline-3,4′-piperidine]hydrochloride used in Example 89 were replaced with the corresponding starting materials of each desired compound.

EXAMPLE 90 1-Methanesulfonyl-N-(3-methoxyphenethyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide

[0341]¹H-NMR(300 MHz, CDCl₃,δppm): 1.64-1.75 (2H,br d,J=13.2 Hz), 1.87 (2H,dt,J=13.2,4.2 Hz), 2.83 (2H,t,J=6.5 Hz), 2.85-2.97 (2H,m), 2.91 (3H,s), 3.51 (1H,t,J=6.5 Hz), 3.53 (1H,t,J=6.5 Hz), 3.79 (3H,s), 3.83 (2H,s), 3.84-3.95 (2H,br d,J=13.5 Hz), 4.48 (1H,t), 6.75-6.81 (3H,m), 7.07 (1H,t,J=7.4 Hz), 7.14 (1H,dd,J=7.4, 1.7 Hz), 7.18-7.30 (2H,m).

EXAMPLE 91 N-(4-Dimethylamino-2-methoxyphenethyl)-1-methanesulfonyl-spiro[indoline-3,4′-piperidine]-1′-carboxamide

[0342]¹H-NMR(300 MHz,CDCl₃,δppm): 1.65-1.78 (2H,m), 2.76 (2H,t,J=6.4 Hz), 2.91 (3H,s), 2.93 (6H,s), 2.80-3.00 (2H,m), 3.42 (1H,t,J=6.4 Hz), 3.44 (1H,t,J=6.4 Hz), 3.83 (5H,s), 3.85-3.97 (2H,m), 4.86-4.95 (1H,m), 6.27 (1H,d,J=2.3 Hz), 6.31 (1H,dd,J=8.4, 2.3 Hz), 6.95-7.20 (4H, m), 7.20-7.30 (2H,m), 7.39 (1H,d,J=6.0 Hz).

EXAMPLE 92 N-[(S)-1-Benzyloxycarbonyl-2-(3-indolyl)ethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H), 4′-piperidine]-1′-carboxamide

[0343]¹H-NMR(300 MHz,CDCl₃,δppm): 1.71 (2H,br d,J=14.3 Hz), 1.91-2.12 (2H,m), 2.82-3.08 (2H,m), 3.30 (1H,dd,J=14.4, 5.0 Hz), 3.38 (1H,dd,J=14.4, 5.0 Hz), 3.63 (2H,s), 3.85 (2H,br d,J=14.3 Hz), 4.91 (1H,dt,J=8.0, 5.0 Hz), 5.01 (1H,d,J=8.0 Hz), 5.14 (1H,d,J=11.9 Hz), 5.22 (1H,d,J=11.9 Hz), 6.34 (1H,br s), 6.65 (1H,s), 7.09 (1H,t,J=6.9 Hz), 7.12-7.40 (11H,m), 7.55 (1H,d,J=8.9 Hz), 7,98 (1H,br s).

EXAMPLE 93 N-[(R)-1-Benzyloxycarbonyl-2-(3-indolyl)ethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide

[0344]¹H-NMR(300 MHz,CDCl₃,δppm): 1.71 (2H,br d,J=14.3 Hz), 1.91-2.12 (2H,m), 2.82-3.08 (2H,m), 3.30 (1H,dd,J=14.4, 5.0 Hz), 3.38 (1H,dd,J=14.4, 5.0 Hz), 3.63 (2H,s), 3.85 (2H,brd,J=14.3 Hz), 4.91 (1H,dt,J=8.0, 5.0 Hz), 5.01 (1H,d,J=8.0 Hz), 5.14 (1H,d,J=11.9 Hz), 5.22 (1H,d,J=11.9 Hz), 6.34 (1H,br s), 6.65 (1H,s), 7.09 (1H,t,J=6.9 Hz), 7.12-7.40 (11H,m), 7.55 (1H,d,J=8.9 Hz), 7,98 (1H,br s).

EXAMPLE 94 N-[(S)-1-Benzyloxycarbonyl-2-cyclohexylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide

[0345]¹H-NMR(300 MHz,CDCl₃,δppm): 0.82-1.00 (2H,m), 1.05-1.41 (5H,m), 1.46-1.81 (6H,m), 1.82 (2H,br d,J=12.1 Hz), 2.05-2.10 (2H,m), 3.05-3.22 (2H,m), 3.66 (2H,s), 4.03 (2H,br t,J=12.1 Hz), 4.60 (1H,dt,J=8.3, 5.6 Hz), 4.93 (1H,d,J=8.3 Hz), 5.11 (1H,d,J=12.4 Hz), 5.24 (1H,d,J=12.4 Hz), 6.70 (1H,br s), 7.12-7.42 (9H,m).

EXAMPLE 95 3,4-Dihydro-N-(3-methoxyphenethyl)-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide

[0346]¹H-NMR(300 MHz,CDCl₃,δppm): 1.75-1.85 (2H,m), 2.02-2.16 (2H,m), 2.83 (2H,t,J=6.8 Hz), 3.02-3.15 (2H,m), 3.52 (1H,t,J=6.8 Hz), 3.54 (1H,t,J=6.8 Hz), 3.66 (2H,s), 3.80 (3H,s), 3.85-3.98 (2H,m), 4.47-4.56 (1H,m), 6.52 (1H,s), 6.72-6.82 (3H,m), 7.15-7.32 (5H,m).

[0347] Industrial Applicability

[0348] Compounds of the present invention have NPY antagonistic actions, therefore they are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, etc., sexual and reproductive dysfunctions, gastro-intestinal disorders such as gastro-intestinal motility disorder, respiratory disorders, inflammatory diseases or glaucoma. 

1. a compound of the formula (i):

(wherein A is a straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of oxo, amino, lower alkylamino, di-lower alkylamino, hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl and —R^(a), and is optionally intervened by oxygen or nitrogen atom; Ar¹ is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar²; Ar² is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl; n is 0 or 1; Q is a single bond or carbonyl; R^(a) is lower alkyl which is optionally substituted by a substituent selected from the group consisting of amino, lower alkylamino, di-lower alkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine; R⁰ is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A; R¹, R² and R⁵ are independently hydrogen, lower alkyl, aralkyl or aryl; R³ and R⁴ are independently hydrogen, hydroxy, lower alkyl, aralkyl or aryl; T, U, V and W are independently methine or nitrogen atom, said methine being optionally substituted by a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, and at least two of T, U, V and W are said methine group; X is —N(SO₂R¹)—, —N(COR²)— or —CO—; Y is —C(R³)(R⁴)—, —O— or —N(R⁵)—; Z is methine or nitrogen atom), or a salt or ester thereof.
 2. The compound as claimed in claim 1, wherein X is —N(SO₂R¹)— or —N(COR²)—, n is 0, and Y is —C(R³)(R⁴)—; or X is —CO—, and Y is —O— or —N(R⁵)—.
 3. The compound as claimed in claim 1, wherein T, U, V and W are independently methine which is optionally substituted by a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy.
 4. The compound as claimed in claim 1, wherein one of T, U, V and W is nitrogen atom.
 5. The compound as claimed in claim 1, wherein X is —CO—, and Y is —O— or —NH—.
 6. The compound as claimed in claim 1, wherein X is —CO—, and Y is —O—.
 7. The compound of the formula (I-a) as claimed in claim 1:

wherein A is a straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of oxo, amino, lower alkylamino, di-lower alkylamino, hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl and —R^(a), and is optionally intervened by oxygen or nitrogen atom; Ar¹ is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar²; Ar² is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl; Q is a single bond or carbonyl; R^(a) is lower alkyl which is optionally substituted by a substituent selected from the group consisting of amino, lower alkylamino, di-lower alkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine; R⁰ is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A; R¹ is hydrogen, lower alkyl, aralkyl or aryl.
 8. The compound of the formula (I-b) as claimed in claim 1:

wherein A is a straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of oxo, amino, lower alkylamino, di-lower alkylamino, hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl and —R^(a), and is optionally intervened by oxygen or nitrogen atom; Ar¹ is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar²; Ar² is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl; Q is a single bond or carbonyl; R^(a) is lower alkyl which is optionally substituted by a substituent selected from the group consisting of amino, lower alkylamino, di-lower alkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine; R⁰ is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A; R¹ is hydrogen, lower alkyl, aralkyl or aryl.
 9. The compound of the formula (I-c) as claimed in claim 1:

wherein A is a straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of oxo, amino, lower alkylamino, di-lower alkylamino, hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl and —R^(a), and is optionally intervened by oxygen or nitrogen atom; Ar¹ is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar²; Ar² is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl; Q is a single bond or carbonyl; R^(a) is lower alkyl which is optionally substituted by a substituent selected from the group consisting of amino, lower alkylamino, di-lower alkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine; R⁰ is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A.
 10. The compound of the formula (I-d) as claimed in claim 1:

wherein A is a straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of oxo, amino, lower alkylamino, di-lower alkylamino, hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl and —R^(a), and is optionally intervened by oxygen or nitrogen atom; Ar¹ is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar² Ar² is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl; Q is a single bond or carbonyl; R^(a) is lower alkyl which is optionally substituted by a substituent selected from the group consisting of amino, lower alkylamino, di-lower alkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine; R⁰ is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A; T, U, V and W are independently methine or nitrogen atom, said methine being optionally substituted by a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, and at least two of T, U, V and W are said methine group.
 11. The compound as claimed in claim 10, wherein all of T, U, V and W are unsubstituted methine.
 12. The compound as claimed in claim 10, wherein one of T, U, V and W is nitrogen atom.
 13. The compound of the formula (I-e) as claimed in claim 1:

wherein A is a straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of oxo, amino, lower alkylamino, di-lower alkylamino, hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl and —R^(a), and is optionally intervened by oxygen or nitrogen atom; Ar¹ is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar²; Ar² is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl; Q is a single bond or carbonyl; R^(a) is lower alkyl which is optionally substituted by a substituent selected from the group consisting of amino, lower alkylamino, di-lower alkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine; R⁰ is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A.
 14. The compound as claimed in claim 1, wherein aryl as Ar¹ is phenyl.
 15. The compound as claimed in claim 1, wherein Ar¹ is heteroaryl which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar².
 16. The compound as claimed in claim 1, selected from the group consisting of: trans-3′-oxo-N-(trans-4-phenylcyclohexyl)spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[(3S)-1-(2-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[(3S)-1-(3-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[(3S)-1-(4-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[1-(2-fluorophenyl)-4-piperidyl]-3′-oxospiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3′-oxospiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[1-(4-fluorophenyl)-4-piperidyl]-3′-oxospiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-3′-oxo-N-(1,2,3,4-tetrahydro-2-naphthyl)spiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[4-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[5-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[6-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[7-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[6-methoxy-1,2,3,4-tetrahydro-2-naphthyl]-3-oxo-spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3′-oxo-N-[(3S)-5-oxo-1-phenyl-3-pyrrolidinyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[(3S)-1-(2-fluorophenyl)-3-pyrrolidinyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[(3S)-1-(3-fluorophenyl)-3-pyrrolidinyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[5-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[6-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[7-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3-oxo-N-[(3S)-1-phenyl-3-pyrrolidinyl]spiro[6-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3-oxo-N-[(3S)-1-(3-trifluoromethylphenyl)3-pyrrolidinyl]spiro[6-aza-isobenzofuran-1(3H),1′-cyclo-hexane]-4′-carboxamide, trans-3-oxo-N-[(3S)-1-(2-pyridyl)-3-pyrrolidinyl]spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3-oxo-N-[(3S)-1-(3-pyridyl)3-pyrrolidinyl]spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[trans-4-(4-fluorophenyl)cyclohexyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxo-spiro[4-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxo-spiro[7-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[(3S)-1-(3,5-difluorophenyl)-3-pyrrolidinyl-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[1-(3,5-difluorophenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[3-(3-fluorophenyl)-tetrahydropyran-6-yl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[trans-4-(2-fluorophenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-benzyl-2-(benzylamino)ethyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-benzhydryl-3′-oxospiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-1-methanesulfonyl-N-(1-phenyl-4-piperidyl)spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-(2-indanyl)-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-1-(3-fluorophenyl)-4-piperidyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-[1-(2-pyridyl)-4-piperidyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-(1-phenyl-3-piperidyl)spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[1-(3,5-difluorophenyl)-3-piperidyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-[1-(2-pyridyl)-3-piperidyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-[(3S)-1-phenyl-3-pyrrolidinyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-[(3R)-1-phenyl-3-pyrrolidinyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-(2-phenylcyclo-propyl)spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-[(2-(3-pyridyl)cyclo-propyl)spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-benzyl-2-(benzylamino)ethyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[1-benzylcarbamoyl-2-(4-pyridyl)ethyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[2-(4-fluorophenyl)-1-[(4-pyridyl-methyl)carbamoyl]ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide trans-N-(2-hydroxy-2-phenylethyl)-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-(benzoylmethyl)-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-benzyl-2-(N-benzylmethylamino)ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-(N-benzylmethylcarbamoyl-2-phenylethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-(N-benzylmethylcarbamoyl)-2-(3-pyridyl)ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-(4-dimethylaminophenethyl)-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-[2-(3-quinolyl)ethyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[2-(4-dimethylaminophenyl)-2-hydroxyethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[2-hydroxy-2-(3-quinolyl)ethyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[2-(3,5-difluorophenyl)-2-hydroxyethyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-benzyl-2-[(3-pyridylmethyl)amino]ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-benzyl-2-[(2-pyridylmethyl)amino]ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-2-anilino-1-benzylethyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-[(S)-1-benzyl-2-(isobutylamino)ethyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-1-methanesulfonyl-N-[2-phenyl-1-(methoxy-carbonyl)ethyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, trans-N-(1-hydroxymethyl-2-phenylethyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide, 1-methanesulfonyl-N-(1-phenyl-4-piperidyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide, 3-oxo-N-(1-phenyl-3-piperidyl)spiro[isobenzofuran-1(3H),4′-piperidine]-1′-carboxamide, 3-oxo-N-[(3S)-1-phenyl-3-pyrrolidinyl]spiro[isobenzofuran-1(3H),4′-piperidine]-1′-carboxamide, N-[1-benzylcarbamoyl-2-cyclohexylethyl]-3,4-dihydro-3-oxo-spiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide, N-[(S)-1-benzyloxymethyl-2-cyclohexylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide, N-[(S)-1-benzylcarbamoyl-2-phenylethyl]-3,4-dihydro-3-oxo-spiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide, N-[(S)-1-benzyl-2-(benzylamino)ethyl]-3,4-dihydro-3-oxo-spiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide, N-(2-indanyl)-1-methanesulfonylspiro[indoline-3,4′-piperidine]-1′-carboxamide, 1-methanesulfonyl-N-phenethylspiro[indoline-3,4′-piperidine]-1′-carboxamide, 1-methanesulfonyl-N-(3-phenylpropyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide, 1-methanesulfonyl-N-(4-phenylbutyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide, N-(4-bromophenethyl)-1-methanesulfonylspiro[indoline-3,4′-piperidine]-1′-carboxamide, N-(3,4-dimethoxyphenethyl)-1-methanesulfonylspiro[indoline-3,4′-piperidine]-1′-carboxamide, 1-methanesulfonyl-N-(3-methoxyphenethyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide, N-(4-dimethylamino-2-methoxyphenethyl)-1-methane-sulfonylspiro[indoline-3,4′-piperidine]-1′-carboxamide, N-[(S)-1-benzyloxycarbonyl-2-(3-indolyl)ethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide, N-[(R)-1-benzyloxycarbonyl-2-(3-indolyl)ethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide, N-[(S)-1-benzyloxycarbonyl-2-cyclohexylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide, 3,4-dihydro-N-(3-methoxyphenethyl)-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-4′-carboxamide, trans-N-[1-(3-trifluoromethylphenyl)-4-piperidyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-N-[trans-2-(3-fluorophenyl)cyclopropyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[trans-2-(4-fluorophenyl)cyclopropyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[1-(2-fluorophenyl)-4-piperidyl]-3-oxospiro[6-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3′-oxo-N-[5-oxo-1-(2-fluorophenyl)-3-pyrrolidinyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-3′-oxo-N-[5-oxo-1-(3-fluorophenyl)-3-pyrrolidinyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-3-oxo-N-[5-oxo-1-(3-fluorophenyl)-3-pyrrolidinyl]spiro[6-azaisobenzofuran-1(3H),1′-cyclo-hexane]-4′-carboxamide, trans-N-[trans-4-(3-trifluoromethylphenyl)cyclohexyl]3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, trans-3′-oxo-N-[2-oxo-1-phenyl-4-piperidyl]spiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-3′-oxo-N-[2-oxo-1-(3-fluorophenyl)-4-piperidyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[trans-2-(2-fluorophenyl)clyclopropyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide, trans-N-[trans-2-(3-fluorophenyl)cyclopropyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide and trans-N-[trans-2-(4-fluorophenyl)cyclopropyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide.
 17. A process for preparing a compound of the formula (I-1):

(wherein A is a straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of oxo, amino, lower alkylamino, di-lower alkylamino, hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl and —R^(a), and is optionally intervened by oxygen or nitrogen atom; Ar¹ is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar²; Ar² is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl; Q is a single bond or carbonyl; R^(a) is lower alkyl which is optionally substituted by a substituent selected from the group consisting of amino, lower alkylamino, di-lower alkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine; T, U, V and W are independently methine or nitrogen atom, said methine being optionally substituted by a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, and at least two of T, U, V and W are said methine group; n, R⁰, X and Y have the same meaning as defined below), or a salt or ester thereof, which comprises reacting a compound of the formula (II):

(wherein A^(p) is a straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of di-lower alkylamino, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl, —R^(ap), optionally protected oxo, optionally protected amino, optionally protected lower alkylamino and optionally protected hydroxy, and is optionally intervened by oxygen or nitrogen atom; Ar^(1p) is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, lower alkyl, halo-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, di-lower alkylamino, lower alkylthio, lower alkanoyl, lower alkoxycarbonyl, -Q^(p)-Ar^(2p), optionally protected oxo, optionally protected hydroxy-lower alkyl optionally protected lower alkylamino and optionally protected carboxyl; Ar^(2p) is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, lower alkoxy, halo-lower alkoxy, di-lower alkylamino, lower alkanoyl, aryl, optionally protected hydroxy-lower alkyl, optionally protected hydroxy and optionally protected lower alkylamino; Ar³ is halogen, or phenyl which is optionally substituted by nitro; Q^(p) is a single bond or optionally protected carbonyl; R^(ap) is lower alkyl which is optionally substituted by a substituent selected from the group consisting of di-lower alkylamino, optionally protected amino, optionally protected lower alkylamino, optionally protected hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine; R^(0p) is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A^(p)) with a compound of the formula (III):

(wherein n is 0 or 1; R¹, R² and R⁵ are independently hydrogen, lower alkyl, aralkyl or aryl; R³ and R⁴ are independently hydrogen, lower alkyl, aralkyl, aryl and optionally protected hydroxy; t, u, v and w are independently methine or nitrogen atom, said methine being optionally substituted by a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy and optionally protected hydroxy, and at least two of t, u, v and w are said methine group; X is —N(SO₂R¹)—, —N(COR²)— or —CO—; Y is —C(R³)(R⁴)—, —O— or —N(R⁵)—) to give a compound of the formula (IV-1):

(wherein A^(p), Ar^(1p), n, R⁰, t, u, v, w, X and Y have the same meaning as defined above), and optionally removing the protecting group(s) from the compound (IV-1).
 18. A process for preparing a compound of the formula (I-2):

(wherein A is a straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of oxo, amino, lower alkylamino, di-lower alkylamino, hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl and —R^(a), and is optionally intervened by oxygen or nitrogen atom; Ar¹ is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar²; Ar² is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl; Q is a single bond or carbonyl; R^(a) is lower alkyl which is optionally substituted by a substituent selected from the group consisting of amino, lower alkylamino, di-lower alkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine; T, U, V and W are independently methine or nitrogen atom, said methine being optionally substituted by a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, and at least two of T, U, V and W are said methine group; n, R⁰, X and Y have the same meaning as defined below), or a salt or ester thereof, which comprises reacting a compound of the formula (V):

(wherein A^(p) is a straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of di-lower alkylamino, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl, —R^(ap), optionally protected oxo, optionally protected amino, optionally protected lower alkylamino and optionally protected hydroxy, and is optionally intervened by oxygen or nitrogen atom; Ar^(1p) is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, lower alkyl, halo-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, di-lower alkylamino, lower alkylthio, lower alkanoyl, lower alkoxycarbonyl, -Q^(p)-Ar² , optionally protected oxo, optionally protected hydroxy-lower alkyl optionally protected lower alkylamino and optionally protected carboxyl; Ar^(2p) is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, lower alkoxy, halo-lower alkoxy, di-lower alkylamino, lower alkanoyl, aryl, optionally protected hydroxy-lower alkyl, optionally protected hydroxy and optionally protected lower alkylamino; Q^(p) is a single bond or optionally protected carbonyl; R^(ap) is lower alkyl which is optionally substituted by a substituent selected from the group consisting of di-lower alkylamino, optionally protected amino, optionally protected lower alkylamino and optionally protected hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine; R^(0p) is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A^(p)) with a compound of the formula (VI):

(wherein n is 0 or 1; R¹, R² and R⁵ are independently hydrogen, lower alkyl, aralkyl or aryl; R³ and R⁴ are independently hydrogen, lower alkyl, aralkyl, aryl and optionally protected hydroxy; t, u, v and w are independently methine or nitrogen atom, said methine being optionally substituted by a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy and optionally protected hydroxy, and at least two of t, u, v and w are said methine group; X is —N(SO₂R¹)—, —N(COR²)— or —CO—; Y is —C(R³)(R⁴)—, —O— or —N(R⁵)—) to give a compound of the formula (IV-2):

(wherein A^(p), Ar^(1p), n, R⁰, t, u, v, w, X and Y have the same meaning as defined above), and optionally removing the protecting group(s) from the compound (IV-2).
 19. A neuropeptide Y receptor antagonist agent comprising a compound of the formula (I):

(wherein A is a straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of oxo, amino, lower alkylamino, di-lower alkylamino, hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl and —R^(a), and is optionally intervened by oxygen or nitrogen atom; Ar¹ is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar²; Ar² is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl; n is 0 or 1; Q is a single bond or carbonyl; R^(a) is lower alkyl which is optionally substituted by a substituent selected from the group consisting of amino, lower alkylamino, di-lower alkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine; R⁰ is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A; R¹, R² and R⁵ are independently hydrogen, lower alkyl, aralkyl or aryl; R³ and R⁴ are independently hydrogen, hydroxy, lower alkyl, aralkyl or aryl; T, U, V and W are independently methine or nitrogen atom, said methine being optionally substituted by a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, and at least two of T, U, V and W are said methine group; X is —N(SO₂R¹)—, —N(COR²)— or —CO—; Y is —C(R³)(R⁴)—, —O— or —N(R⁵)—; Z is methine or nitrogen atom), or a salt or ester thereof as an active ingredient.
 20. An agent for the treatment of bulimia, obesity or diabetes, comprising a compound of the formula (I):

(wherein A is a straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally substituted by a substituent selected from the group consisting of oxo, amino, lower alkylamino, di-lower alkylamino, hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl and —R^(a), and is optionally intervened by oxygen or nitrogen atom; Ar¹ is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl and -Q-Ar²; Ar² is aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy, halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl; n is 0 or 1; Q is a single bond or carbonyl; R^(a) is lower alkyl which is optionally substituted by a substituent selected from the group consisting of amino, lower alkylamino, di-lower alkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the last three groups being optionally substituted by fluorine; R⁰ is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A; R¹, R² and R⁵ are independently hydrogen, lower alkyl, aralkyl or aryl; R³ and R⁴ are independently hydrogen, hydroxy, lower alkyl, aralkyl or aryl; T, U, V and W are independently methine or nitrogen atom, said methine being optionally substituted by a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, and at least two of T, U, V and W are said methine group; X is 13 N(SO₂R¹)—, —N(COR²)— or —CO—; Y is —C(R³)(R⁴)—, —O— or —N(R⁵)—; Z is methine or nitrogen atom), or a salt or ester thereof as an active ingredient.
 21. The compound or salt thereof of claim 1, wherein the compound is trans-3′-oxo-N-(trans-4-phenylcyclohexyl)-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide.
 22. The compound or salt thereof of claim 1, wherein the compound is trans-N-[1-(2-fluorophenyl)-4-piperidyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide.
 23. The compound or salt thereof of claim 1, wherein the compound is trans-N-[1-(3-fluorophenyl)-4-piperidyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide.
 24. The compound or salt thereof of claim 1, wherein the compound is trans-N-[1-(4-fluorophenyl)-4-piperidyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide.
 25. The compound or salt thereof of claim 1, wherein the compound is trans-N-[1-(3,5-difluorophenyl)-4-piperidyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide.
 26. The compound or salt thereof of claim 1, wherein the compound is trans-N-[1-(3,5-difluorophenyl)-4-piperidyl]-3-oxospiro[4-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide. 